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abiraterone acetate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antiandrogens | 4176 | 154229-18-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 alpha-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis. CYP17 catalyzes two sequential reactions: 1) the conversion of pregnenolone and progesterone to their 17alpha-hydroxy derivatives by 17alpha-hydroxylase activity and 2) the subsequent formation of dehydroepiandrosterone (DHEA) and androstenedione, respectively, by C17,20 lyase activity. DHEA and androstenedione are androgens and are precursors of testosterone. Inhibition of CYP17 by abiraterone can also result in increased mineralocorticoid production by the adrenals. Androgen sensitive prostatic carcinoma responds to treatment that decreases androgen levels. Androgen deprivation therapies, such as treatment with GnRH agonists or orchiectomy, decrease androgen production in the testes but do not affect androgen production by the adrenals or in the tumor. Abiraterone acetate decreased serum testosterone and other androgens in patients in the placebo-controlled clinical trial. It is not necessary to monitor the effect of abiraterone acetate on serum testosterone levels.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.00 mg/mL | Bocci G, Oprea TI, Benet LZ |
| S (Water solubility) | 0.00 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 10 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.698 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.883 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 7.852 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 58.749 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.510 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.390 | % | High | 1 |
| herg | hERG pIC50 | 5.186 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 133.660 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 262.422 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.670 | % | High | 1 |
| kinase-safety-class | ACVR2B,BRAF,EIF2AK3,GRK2,ITK,PDK1,PDK2,PDK4 | 8 | |||
| kinase-selectivity-class | GRK2 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.372 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 269.774 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.610 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.630 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.440 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 271.019 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 3.040 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.700 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 3.532 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 5, 2011 | EMA | Janssen-Cilag International N.V. | |
| April 28, 2011 | FDA | JANSSEN BIOTECH |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Prostatic specific antigen increased | 59.52 | 36.86 | 5 | 223 | 0 | 90628219 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Prostatic specific antigen increased | 2451.50 | 16.03 | 861 | 46846 | 16064 | 42557564 |
| Death | 2409.39 | 16.03 | 2772 | 44935 | 468413 | 42105215 |
| Hot flush | 816.89 | 16.03 | 429 | 47278 | 21922 | 42551706 |
| Disease progression | 742.93 | 16.03 | 857 | 46850 | 142799 | 42430829 |
| Therapy cessation | 700.58 | 16.03 | 376 | 47331 | 20074 | 42553554 |
| Hypokalaemia | 681.90 | 16.03 | 596 | 47111 | 71125 | 42502503 |
| Hospitalisation | 555.38 | 16.03 | 540 | 47167 | 73790 | 42499838 |
| Metastases to bone | 500.68 | 16.03 | 270 | 47437 | 14539 | 42559089 |
| Prostate cancer metastatic | 463.34 | 16.03 | 199 | 47508 | 6430 | 42567198 |
| Fatigue | 315.12 | 16.03 | 1134 | 46573 | 434507 | 42139121 |
| Osteonecrosis of jaw | 296.64 | 16.03 | 212 | 47495 | 18837 | 42554791 |
| Malignant neoplasm progression | 245.35 | 16.03 | 437 | 47270 | 107963 | 42465665 |
| Prostate cancer | 234.28 | 16.03 | 269 | 47438 | 44374 | 42529254 |
| Urinary tract infection | 232.08 | 16.03 | 406 | 47301 | 98878 | 42474750 |
| Therapy interrupted | 183.58 | 16.03 | 171 | 47536 | 22079 | 42551549 |
| Product size issue | 167.96 | 16.03 | 54 | 47653 | 751 | 42572877 |
| Rhabdomyolysis | 154.34 | 16.03 | 297 | 47410 | 77722 | 42495906 |
| Hormone-refractory prostate cancer | 152.39 | 16.03 | 53 | 47654 | 951 | 42572677 |
| Hypertension | 143.43 | 16.03 | 462 | 47245 | 166742 | 42406886 |
| Hospice care | 142.35 | 16.03 | 99 | 47608 | 8414 | 42565214 |
| Product use complaint | 139.68 | 16.03 | 62 | 47645 | 2169 | 42571459 |
| Adverse event | 138.61 | 16.03 | 151 | 47556 | 23489 | 42550139 |
| Bone pain | 127.50 | 16.03 | 145 | 47562 | 23647 | 42549981 |
| Blood potassium decreased | 120.89 | 16.03 | 131 | 47576 | 20253 | 42553375 |
| Acquired apparent mineralocorticoid excess | 117.37 | 16.03 | 26 | 47681 | 68 | 42573560 |
| Prostatic specific antigen abnormal | 110.93 | 16.03 | 41 | 47666 | 883 | 42572745 |
| Oedema peripheral | 101.56 | 16.03 | 359 | 47348 | 135717 | 42437911 |
| Dysphagia | 100.09 | 16.03 | 239 | 47468 | 72480 | 42501148 |
| Toxicity to various agents | 93.37 | 16.03 | 72 | 47635 | 229064 | 42344564 |
| Spinal cord compression | 89.66 | 16.03 | 57 | 47650 | 4167 | 42569461 |
| Completed suicide | 87.72 | 16.03 | 5 | 47702 | 96460 | 42477168 |
| Prescribed underdose | 86.67 | 16.03 | 80 | 47627 | 10202 | 42563426 |
| Decreased appetite | 86.55 | 16.03 | 436 | 47271 | 192701 | 42380927 |
| Hepatotoxicity | 85.09 | 16.03 | 122 | 47585 | 25045 | 42548583 |
| Asthenia | 82.51 | 16.03 | 567 | 47140 | 280226 | 42293402 |
| Apparent mineralocorticoid excess | 78.47 | 16.03 | 18 | 47689 | 58 | 42573570 |
| Metastases to lymph nodes | 78.16 | 16.03 | 60 | 47647 | 5938 | 42567690 |
| Haematuria | 75.28 | 16.03 | 186 | 47521 | 57613 | 42516015 |
| Blood alkaline phosphatase increased | 75.25 | 16.03 | 135 | 47572 | 33462 | 42540166 |
| Fall | 72.69 | 16.03 | 480 | 47227 | 234040 | 42339588 |
| Hyperaldosteronism | 70.55 | 16.03 | 21 | 47686 | 222 | 42573406 |
| Hepatic function abnormal | 68.26 | 16.03 | 167 | 47540 | 51400 | 42522228 |
| Metabolic alkalosis | 67.33 | 16.03 | 37 | 47670 | 2064 | 42571564 |
| Metastases to spine | 66.50 | 16.03 | 42 | 47665 | 3035 | 42570593 |
| Pyrexia | 63.10 | 16.03 | 228 | 47479 | 393814 | 42179814 |
| Pruritus | 61.99 | 16.03 | 72 | 47635 | 188699 | 42384929 |
| Febrile neutropenia | 60.79 | 16.03 | 71 | 47636 | 185632 | 42387996 |
| Metastases to liver | 59.42 | 16.03 | 82 | 47625 | 16244 | 42557384 |
| Metastases to lung | 58.45 | 16.03 | 68 | 47639 | 11356 | 42562272 |
| Acquired haemophilia | 57.85 | 16.03 | 31 | 47676 | 1644 | 42571984 |
| Muscular weakness | 56.07 | 16.03 | 213 | 47494 | 83285 | 42490343 |
| Anaemia | 55.92 | 16.03 | 518 | 47189 | 279760 | 42293868 |
| Incorrect dose administered | 55.27 | 16.03 | 157 | 47550 | 52817 | 42520811 |
| Acute coronary syndrome | 54.61 | 16.03 | 75 | 47632 | 14790 | 42558838 |
| Condition aggravated | 54.60 | 16.03 | 133 | 47574 | 260621 | 42313007 |
| Cardiac failure | 54.10 | 16.03 | 250 | 47457 | 106606 | 42467022 |
| Urinary tract obstruction | 54.01 | 16.03 | 41 | 47666 | 3990 | 42569638 |
| Drug hypersensitivity | 52.08 | 16.03 | 23 | 47684 | 99366 | 42474262 |
| Oedema | 50.29 | 16.03 | 150 | 47557 | 51851 | 42521777 |
| Hydronephrosis | 49.95 | 16.03 | 64 | 47643 | 11801 | 42561827 |
| Chemotherapy | 49.15 | 16.03 | 22 | 47685 | 785 | 42572843 |
| Fluid retention | 49.06 | 16.03 | 109 | 47598 | 31510 | 42542118 |
| Intentional product use issue | 47.57 | 16.03 | 11 | 47696 | 71822 | 42501806 |
| Infusion related reaction | 47.53 | 16.03 | 6 | 47701 | 60800 | 42512828 |
| Wheezing | 46.43 | 16.03 | 4 | 47703 | 54777 | 42518851 |
| Product dose omission issue | 45.96 | 16.03 | 313 | 47394 | 154052 | 42419576 |
| Prostate cancer recurrent | 45.91 | 16.03 | 23 | 47684 | 1060 | 42572568 |
| Intentional overdose | 45.76 | 16.03 | 3 | 47704 | 51453 | 42522175 |
| Overdose | 45.51 | 16.03 | 31 | 47676 | 105233 | 42468395 |
| Hypotension | 45.29 | 16.03 | 143 | 47564 | 257488 | 42316140 |
| Asthma | 44.47 | 16.03 | 8 | 47699 | 62306 | 42511322 |
| BRCA2 gene mutation | 43.31 | 16.03 | 11 | 47696 | 60 | 42573568 |
| Liver function test abnormal | 42.96 | 16.03 | 105 | 47602 | 32286 | 42541342 |
| Therapy change | 42.79 | 16.03 | 36 | 47671 | 4059 | 42569569 |
| Back pain | 41.92 | 16.03 | 287 | 47420 | 141489 | 42432139 |
| Bone lesion | 41.53 | 16.03 | 33 | 47674 | 3433 | 42570195 |
| Haemorrhage urinary tract | 41.43 | 16.03 | 27 | 47680 | 2059 | 42571569 |
| Injection site pain | 40.01 | 16.03 | 8 | 47699 | 57790 | 42515838 |
| Psoriasis | 39.99 | 16.03 | 4 | 47703 | 48600 | 42525028 |
| Diabetes mellitus | 39.27 | 16.03 | 152 | 47555 | 59935 | 42513693 |
| Hepatic enzyme increased | 38.66 | 16.03 | 126 | 47581 | 45658 | 42527970 |
| Metastasis | 38.47 | 16.03 | 36 | 47671 | 4669 | 42568959 |
| Blood urine present | 38.37 | 16.03 | 56 | 47651 | 11677 | 42561951 |
| BRCA1 gene mutation | 38.02 | 16.03 | 10 | 47697 | 64 | 42573564 |
| Wrong technique in product usage process | 37.51 | 16.03 | 119 | 47588 | 42516 | 42531112 |
| Neuroendocrine carcinoma of prostate | 36.78 | 16.03 | 9 | 47698 | 41 | 42573587 |
| Off label use | 36.50 | 16.03 | 500 | 47207 | 637835 | 41935793 |
| Plasma cell myeloma | 36.45 | 16.03 | 5 | 47702 | 47573 | 42526055 |
| Anxiety | 35.97 | 16.03 | 48 | 47659 | 118512 | 42455116 |
| Coma | 35.86 | 16.03 | 8 | 47699 | 53546 | 42520082 |
| Aggression | 35.40 | 16.03 | 4 | 47703 | 44159 | 42529469 |
| Agitation | 35.10 | 16.03 | 14 | 47693 | 64300 | 42509328 |
| Hereditary optic atrophy | 33.77 | 16.03 | 9 | 47698 | 61 | 42573567 |
| Urinary retention | 33.70 | 16.03 | 114 | 47593 | 42100 | 42531528 |
| Rheumatoid arthritis | 33.63 | 16.03 | 4 | 47703 | 42436 | 42531192 |
| Hypoxia | 32.29 | 16.03 | 19 | 47688 | 69767 | 42503861 |
| Polyneuropathy in malignant disease | 32.02 | 16.03 | 13 | 47694 | 363 | 42573265 |
| Lactic acidosis | 31.88 | 16.03 | 6 | 47701 | 45255 | 42528373 |
| Intentional product misuse | 31.36 | 16.03 | 15 | 47692 | 61885 | 42511743 |
| Adrenal insufficiency | 31.36 | 16.03 | 67 | 47640 | 18857 | 42554771 |
| Erythema | 31.05 | 16.03 | 46 | 47661 | 108747 | 42464881 |
| Torsade de pointes | 29.53 | 16.03 | 42 | 47665 | 8552 | 42565076 |
| Oxygen saturation decreased | 29.38 | 16.03 | 18 | 47689 | 64669 | 42508959 |
| Product use in unapproved indication | 29.24 | 16.03 | 107 | 47600 | 184349 | 42389279 |
| Alanine aminotransferase increased | 29.16 | 16.03 | 184 | 47523 | 88222 | 42485406 |
| Cardiac disorder | 28.94 | 16.03 | 120 | 47587 | 48812 | 42524816 |
| Peripheral swelling | 28.62 | 16.03 | 186 | 47521 | 90084 | 42483544 |
| Prostatic specific antigen decreased | 28.12 | 16.03 | 10 | 47697 | 192 | 42573436 |
| Contusion | 28.07 | 16.03 | 107 | 47600 | 41878 | 42531750 |
| Pathological fracture | 27.90 | 16.03 | 32 | 47675 | 5261 | 42568367 |
| No adverse event | 27.86 | 16.03 | 5 | 47702 | 39016 | 42534612 |
| Acute biphenotypic leukaemia | 27.55 | 16.03 | 8 | 47699 | 77 | 42573551 |
| Cystitis | 27.46 | 16.03 | 48 | 47659 | 11650 | 42561978 |
| Constipation | 27.43 | 16.03 | 290 | 47417 | 162001 | 42411627 |
| Atrial fibrillation | 27.25 | 16.03 | 257 | 47450 | 139336 | 42434292 |
| Cough | 27.13 | 16.03 | 105 | 47602 | 177998 | 42395630 |
| Fracture | 26.97 | 16.03 | 39 | 47668 | 8064 | 42565564 |
| Staphylococcal infection | 26.49 | 16.03 | 5 | 47702 | 37638 | 42535990 |
| Urosepsis | 25.84 | 16.03 | 54 | 47653 | 14966 | 42558662 |
| Pollakiuria | 25.74 | 16.03 | 69 | 47638 | 22436 | 42551192 |
| Metabolic acidosis | 25.62 | 16.03 | 13 | 47694 | 51845 | 42521783 |
| Depressed level of consciousness | 25.27 | 16.03 | 11 | 47696 | 47959 | 42525669 |
| Haemorrhage subcutaneous | 25.08 | 16.03 | 22 | 47685 | 2624 | 42571004 |
| Mucosal inflammation | 24.96 | 16.03 | 12 | 47695 | 49362 | 42524266 |
| Spinal cord infarction | 24.91 | 16.03 | 13 | 47694 | 653 | 42572975 |
| Tachycardia | 24.90 | 16.03 | 47 | 47660 | 101040 | 42472588 |
| Multiple organ dysfunction syndrome | 24.90 | 16.03 | 44 | 47663 | 96991 | 42476637 |
| Cerebrovascular accident | 24.83 | 16.03 | 190 | 47517 | 96970 | 42476658 |
| Myocardial infarction | 24.54 | 16.03 | 229 | 47478 | 123780 | 42449848 |
| Therapeutic product effect incomplete | 24.41 | 16.03 | 26 | 47681 | 70913 | 42502715 |
| Hypersensitivity | 24.37 | 16.03 | 27 | 47680 | 72343 | 42501285 |
| Rash | 24.28 | 16.03 | 196 | 47511 | 276758 | 42296870 |
| Radiotherapy | 23.98 | 16.03 | 14 | 47693 | 877 | 42572751 |
| Suicidal ideation | 23.90 | 16.03 | 12 | 47695 | 48149 | 42525479 |
| Sedation | 23.83 | 16.03 | 3 | 47704 | 30472 | 42543156 |
| Hyperglycaemia | 23.70 | 16.03 | 108 | 47599 | 45751 | 42527877 |
| Drug ineffective for unapproved indication | 23.67 | 16.03 | 11 | 47696 | 46152 | 42527476 |
| Bone cancer metastatic | 23.48 | 16.03 | 9 | 47698 | 215 | 42573413 |
| Free prostate-specific antigen increased | 23.19 | 16.03 | 4 | 47703 | 0 | 42573628 |
| Sinusitis | 23.14 | 16.03 | 12 | 47695 | 47280 | 42526348 |
| Pelvic pain | 23.03 | 16.03 | 23 | 47684 | 3231 | 42570397 |
| Somnolence | 22.91 | 16.03 | 81 | 47626 | 141024 | 42432604 |
| Groin pain | 22.72 | 16.03 | 31 | 47676 | 6073 | 42567555 |
| Hip fracture | 22.67 | 16.03 | 48 | 47659 | 13424 | 42560204 |
| Anaphylactic reaction | 22.21 | 16.03 | 10 | 47697 | 42733 | 42530895 |
| C-reactive protein increased | 22.20 | 16.03 | 23 | 47684 | 63537 | 42510091 |
| Stress | 21.96 | 16.03 | 11 | 47696 | 44201 | 42529427 |
| Liver disorder | 21.72 | 16.03 | 95 | 47612 | 39549 | 42534079 |
| Aspartate aminotransferase increased | 21.48 | 16.03 | 154 | 47553 | 77009 | 42496619 |
| Respiratory distress | 21.39 | 16.03 | 10 | 47697 | 41810 | 42531818 |
| Productive cough | 21.21 | 16.03 | 16 | 47691 | 51551 | 42522077 |
| Blood testosterone increased | 21.13 | 16.03 | 16 | 47691 | 1551 | 42572077 |
| Blood creatinine increased | 20.77 | 16.03 | 59 | 47648 | 109944 | 42463684 |
| Skin lesion | 20.48 | 16.03 | 3 | 47704 | 27171 | 42546457 |
| Peri-implantitis | 20.21 | 16.03 | 7 | 47700 | 124 | 42573504 |
| Metastases to soft tissue | 20.20 | 16.03 | 10 | 47697 | 449 | 42573179 |
| Drug reaction with eosinophilia and systemic symptoms | 20.11 | 16.03 | 11 | 47696 | 42064 | 42531564 |
| Musculoskeletal stiffness | 20.06 | 16.03 | 21 | 47686 | 57744 | 42515884 |
| Neutropenia | 19.92 | 16.03 | 136 | 47571 | 199295 | 42374333 |
| Nasopharyngitis | 19.87 | 16.03 | 40 | 47667 | 83956 | 42489672 |
| Loss of personal independence in daily activities | 19.80 | 16.03 | 16 | 47691 | 49800 | 42523828 |
| Retroperitoneal lymphadenopathy | 19.60 | 16.03 | 13 | 47694 | 1021 | 42572607 |
| Pancytopenia | 19.51 | 16.03 | 67 | 47640 | 117676 | 42455952 |
| Colitis ulcerative | 19.47 | 16.03 | 3 | 47704 | 26172 | 42547456 |
| Hypocalcaemia | 19.43 | 16.03 | 76 | 47631 | 30097 | 42543531 |
| Adverse drug reaction | 19.22 | 16.03 | 88 | 47619 | 37346 | 42536282 |
| Bradycardia | 19.13 | 16.03 | 42 | 47665 | 85442 | 42488186 |
| Dizziness | 18.76 | 16.03 | 387 | 47320 | 248867 | 42324761 |
| Gastroduodenal ulcer | 18.63 | 16.03 | 11 | 47696 | 704 | 42572924 |
| Nasal congestion | 18.59 | 16.03 | 5 | 47702 | 29496 | 42544132 |
| Dehydration | 18.47 | 16.03 | 241 | 47466 | 141526 | 42432102 |
| General physical health deterioration | 18.42 | 16.03 | 254 | 47453 | 150992 | 42422636 |
| Pyelonephritis acute | 18.31 | 16.03 | 18 | 47689 | 2482 | 42571146 |
| Eosinophilia | 18.21 | 16.03 | 7 | 47700 | 32892 | 42540736 |
| White blood cell count decreased | 18.17 | 16.03 | 63 | 47644 | 110333 | 42463295 |
| Cancer pain | 17.86 | 16.03 | 21 | 47686 | 3546 | 42570082 |
| Transaminases increased | 17.40 | 16.03 | 78 | 47629 | 32807 | 42540821 |
| Dementia | 17.33 | 16.03 | 49 | 47658 | 16431 | 42557197 |
| Gastrointestinal tube insertion | 17.29 | 16.03 | 14 | 47693 | 1496 | 42572132 |
| Surgery | 17.19 | 16.03 | 51 | 47656 | 17565 | 42556063 |
| Tremor | 16.85 | 16.03 | 54 | 47653 | 96875 | 42476753 |
| Anaphylactic shock | 16.81 | 16.03 | 3 | 47704 | 23514 | 42550114 |
| Urinary bladder haemorrhage | 16.80 | 16.03 | 15 | 47692 | 1832 | 42571796 |
| Cardiotoxicity | 16.77 | 16.03 | 30 | 47677 | 7415 | 42566213 |
| Lymphoedema | 16.73 | 16.03 | 24 | 47683 | 4924 | 42568704 |
| Chills | 16.64 | 16.03 | 52 | 47655 | 94014 | 42479614 |
| Allodynia | 16.61 | 16.03 | 12 | 47695 | 1082 | 42572546 |
| Abdominal pain | 16.58 | 16.03 | 135 | 47572 | 190336 | 42383292 |
| Upper respiratory tract infection | 16.20 | 16.03 | 14 | 47693 | 42159 | 42531469 |
| Rib fracture | 16.20 | 16.03 | 48 | 47659 | 16523 | 42557105 |
| White blood cell count increased | 16.10 | 16.03 | 16 | 47691 | 45071 | 42528557 |
| Heat illness | 16.06 | 16.03 | 8 | 47699 | 364 | 42573264 |
| Toxic cataract | 16.04 | 16.03 | 4 | 47703 | 20 | 42573608 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Prostatic specific antigen increased | 2510.98 | 17.58 | 616 | 33899 | 11895 | 110542889 |
| Death | 1699.92 | 17.58 | 1533 | 32982 | 697336 | 109857448 |
| Disease progression | 706.15 | 17.58 | 594 | 33921 | 243440 | 110311344 |
| Hot flush | 560.35 | 17.58 | 313 | 34202 | 65723 | 110489061 |
| Hypokalaemia | 535.29 | 17.58 | 448 | 34067 | 182000 | 110372784 |
| Metastases to bone | 468.88 | 17.58 | 218 | 34297 | 31154 | 110523630 |
| Prostate cancer metastatic | 443.77 | 17.58 | 129 | 34386 | 4814 | 110549970 |
| Prostate cancer | 399.20 | 17.58 | 207 | 34308 | 37434 | 110517350 |
| Therapy cessation | 319.97 | 17.58 | 190 | 34325 | 44667 | 110510117 |
| Rhabdomyolysis | 318.77 | 17.58 | 279 | 34236 | 120122 | 110434662 |
| Osteonecrosis of jaw | 300.40 | 17.58 | 187 | 34328 | 47830 | 110506954 |
| Hospitalisation | 219.84 | 17.58 | 246 | 34269 | 142247 | 110412537 |
| Malignant neoplasm progression | 212.50 | 17.58 | 267 | 34248 | 174300 | 110380484 |
| Fatigue | 205.21 | 17.58 | 834 | 33681 | 1215124 | 109339660 |
| Haematuria | 155.66 | 17.58 | 159 | 34356 | 82846 | 110471938 |
| Urinary tract infection | 147.77 | 17.58 | 319 | 34196 | 325963 | 110228821 |
| Hormone-refractory prostate cancer | 133.80 | 17.58 | 35 | 34480 | 875 | 110553909 |
| Hospice care | 121.94 | 17.58 | 65 | 34450 | 12408 | 110542376 |
| Product size issue | 118.76 | 17.58 | 32 | 34483 | 899 | 110553885 |
| Oedema peripheral | 106.23 | 17.58 | 282 | 34233 | 328378 | 110226406 |
| Acquired apparent mineralocorticoid excess | 101.93 | 17.58 | 19 | 34496 | 86 | 110554698 |
| Apparent mineralocorticoid excess | 100.48 | 17.58 | 18 | 34497 | 62 | 110554722 |
| Blood potassium decreased | 100.23 | 17.58 | 103 | 34412 | 54011 | 110500773 |
| Prostate cancer recurrent | 99.30 | 17.58 | 28 | 34487 | 934 | 110553850 |
| Infusion related reaction | 95.22 | 17.58 | 6 | 34509 | 381156 | 110173628 |
| Anaemia | 89.81 | 17.58 | 373 | 34142 | 546713 | 110008071 |
| Decreased appetite | 89 | 17.58 | 338 | 34177 | 475508 | 110079276 |
| Therapy interrupted | 85.41 | 17.58 | 91 | 34424 | 49731 | 110505053 |
| Drug hypersensitivity | 84.76 | 17.58 | 19 | 34496 | 454071 | 110100713 |
| Drug interaction | 84.42 | 17.58 | 344 | 34171 | 499839 | 110054945 |
| Cardiac failure | 83.17 | 17.58 | 182 | 34333 | 187444 | 110367340 |
| Asthenia | 82.99 | 17.58 | 429 | 34086 | 688570 | 109866214 |
| Metastases to spine | 82.48 | 17.58 | 38 | 34477 | 5305 | 110549479 |
| Acute kidney injury | 80.97 | 17.58 | 402 | 34113 | 635028 | 109919756 |
| Rheumatoid arthritis | 77.02 | 17.58 | 4 | 34511 | 299609 | 110255175 |
| Bone pain | 76.57 | 17.58 | 98 | 34417 | 65035 | 110489749 |
| Product use complaint | 74.62 | 17.58 | 32 | 34483 | 3771 | 110551013 |
| Urinary retention | 74.40 | 17.58 | 100 | 34415 | 69583 | 110485201 |
| Acute coronary syndrome | 74.36 | 17.58 | 60 | 34455 | 23052 | 110531732 |
| Atrial fibrillation | 74.09 | 17.58 | 197 | 34318 | 229445 | 110325339 |
| Hypersensitivity | 73.22 | 17.58 | 18 | 34497 | 403980 | 110150804 |
| Metastases to liver | 72.21 | 17.58 | 71 | 34444 | 35315 | 110519469 |
| Hyperaldosteronism | 71.88 | 17.58 | 20 | 34495 | 635 | 110554149 |
| Arthropathy | 70.40 | 17.58 | 5 | 34510 | 287517 | 110267267 |
| Metastases to lung | 68.18 | 17.58 | 57 | 34458 | 23006 | 110531778 |
| Wheezing | 66.91 | 17.58 | 3 | 34512 | 255227 | 110299557 |
| Acquired haemophilia | 64.67 | 17.58 | 26 | 34489 | 2605 | 110552179 |
| Incorrect dose administered | 63.32 | 17.58 | 115 | 34400 | 103526 | 110451258 |
| Metabolic alkalosis | 62.83 | 17.58 | 32 | 34483 | 5563 | 110549221 |
| Prostatic specific antigen abnormal | 62.17 | 17.58 | 18 | 34497 | 661 | 110554123 |
| Myocardial infarction | 62.16 | 17.58 | 165 | 34350 | 191918 | 110362866 |
| Metastases to lymph nodes | 61.46 | 17.58 | 45 | 34470 | 14987 | 110539797 |
| Hydronephrosis | 60.94 | 17.58 | 51 | 34464 | 20614 | 110534170 |
| Fall | 60.05 | 17.58 | 357 | 34158 | 603125 | 109951659 |
| Pruritus | 58.71 | 17.58 | 57 | 34458 | 581503 | 109973281 |
| Sinusitis | 58.26 | 17.58 | 11 | 34504 | 296677 | 110258107 |
| Wound | 57.61 | 17.58 | 4 | 34511 | 234433 | 110320351 |
| Blood alkaline phosphatase increased | 57.03 | 17.58 | 89 | 34426 | 70846 | 110483938 |
| Hepatic function abnormal | 55.71 | 17.58 | 100 | 34415 | 89195 | 110465589 |
| Completed suicide | 54.51 | 17.58 | 6 | 34509 | 242375 | 110312409 |
| Asthma | 54.30 | 17.58 | 7 | 34508 | 250284 | 110304500 |
| Intentional product use issue | 53.63 | 17.58 | 7 | 34508 | 247899 | 110306885 |
| Back pain | 53.16 | 17.58 | 243 | 34272 | 370753 | 110184031 |
| Haemorrhage urinary tract | 52.05 | 17.58 | 23 | 34492 | 2913 | 110551871 |
| Bone lesion | 50.44 | 17.58 | 30 | 34485 | 7057 | 110547727 |
| Dehydration | 50.07 | 17.58 | 196 | 34319 | 279315 | 110275469 |
| Neuroendocrine carcinoma of prostate | 49.80 | 17.58 | 9 | 34506 | 33 | 110554751 |
| Spinal cord compression | 48.68 | 17.58 | 30 | 34485 | 7522 | 110547262 |
| Toxicity to various agents | 48.60 | 17.58 | 47 | 34468 | 480508 | 110074276 |
| Alopecia | 48.10 | 17.58 | 27 | 34488 | 364726 | 110190058 |
| Nasopharyngitis | 48.09 | 17.58 | 32 | 34483 | 394329 | 110160455 |
| Constipation | 45.19 | 17.58 | 226 | 34289 | 357560 | 110197224 |
| Urinary tract obstruction | 45.10 | 17.58 | 25 | 34490 | 5152 | 110549632 |
| Polyneuropathy in malignant disease | 44.63 | 17.58 | 13 | 34502 | 488 | 110554296 |
| Hereditary optic atrophy | 42.66 | 17.58 | 9 | 34506 | 84 | 110554700 |
| Musculoskeletal stiffness | 42.58 | 17.58 | 17 | 34498 | 279805 | 110274979 |
| Condition aggravated | 40.99 | 17.58 | 107 | 34408 | 734729 | 109820055 |
| Dysphagia | 40.92 | 17.58 | 123 | 34392 | 153477 | 110401307 |
| Exposure during pregnancy | 40.72 | 17.58 | 3 | 34512 | 167421 | 110387363 |
| Hormone-dependent prostate cancer | 40.16 | 17.58 | 10 | 34505 | 204 | 110554580 |
| Migraine | 39.23 | 17.58 | 4 | 34511 | 171648 | 110383136 |
| Therapy change | 38.78 | 17.58 | 29 | 34486 | 9968 | 110544816 |
| Drug intolerance | 38.55 | 17.58 | 42 | 34473 | 406470 | 110148314 |
| Torsade de pointes | 38.23 | 17.58 | 41 | 34474 | 22559 | 110532225 |
| Blood urine present | 37.57 | 17.58 | 42 | 34473 | 24203 | 110530581 |
| Muscular weakness | 37.24 | 17.58 | 165 | 34350 | 248303 | 110306481 |
| Anxiety | 36.95 | 17.58 | 32 | 34483 | 345046 | 110209738 |
| Hypertension | 36.94 | 17.58 | 279 | 34236 | 509805 | 110044979 |
| Liver function test abnormal | 36.51 | 17.58 | 72 | 34443 | 68878 | 110485906 |
| Syncope | 36.23 | 17.58 | 142 | 34373 | 202394 | 110352390 |
| Blood glucose increased | 35.19 | 17.58 | 106 | 34409 | 132390 | 110422394 |
| Spinal cord infarction | 34.61 | 17.58 | 13 | 34502 | 1085 | 110553699 |
| Inflammation | 34.23 | 17.58 | 9 | 34506 | 193229 | 110361555 |
| Diabetes mellitus | 33.79 | 17.58 | 87 | 34428 | 99294 | 110455490 |
| Osteoarthritis | 33.32 | 17.58 | 8 | 34507 | 182615 | 110372169 |
| Product dose omission issue | 32.98 | 17.58 | 192 | 34323 | 321590 | 110233194 |
| Pollakiuria | 32.16 | 17.58 | 53 | 34462 | 44142 | 110510642 |
| Injection site pain | 32.06 | 17.58 | 8 | 34507 | 177914 | 110376870 |
| Prescribed underdose | 32.06 | 17.58 | 66 | 34449 | 65108 | 110489676 |
| Metastases to nervous system | 32.01 | 17.58 | 9 | 34506 | 297 | 110554487 |
| Acute biphenotypic leukaemia | 31.95 | 17.58 | 8 | 34507 | 167 | 110554617 |
| Rash | 31.80 | 17.58 | 140 | 34375 | 820824 | 109733960 |
| Discomfort | 31.13 | 17.58 | 14 | 34501 | 214693 | 110340091 |
| Prostatic specific antigen decreased | 30.92 | 17.58 | 7 | 34508 | 93 | 110554691 |
| Cerebrovascular accident | 30.73 | 17.58 | 125 | 34390 | 181159 | 110373625 |
| Intentional overdose | 30.50 | 17.58 | 3 | 34512 | 132498 | 110422286 |
| Ill-defined disorder | 30.39 | 17.58 | 6 | 34509 | 156847 | 110397937 |
| Stomatitis | 30.23 | 17.58 | 24 | 34491 | 270218 | 110284566 |
| Blood cholesterol increased | 30.18 | 17.58 | 10 | 34505 | 184775 | 110370009 |
| Psoriasis | 30.15 | 17.58 | 4 | 34511 | 139989 | 110414795 |
| Alanine aminotransferase increased | 29.80 | 17.58 | 125 | 34390 | 183648 | 110371136 |
| Hypocalcaemia | 29.60 | 17.58 | 64 | 34451 | 65302 | 110489482 |
| Therapeutic product effect decreased | 29.53 | 17.58 | 20 | 34495 | 244296 | 110310488 |
| Rib fracture | 29.43 | 17.58 | 44 | 34471 | 33726 | 110521058 |
| Chemotherapy | 29.23 | 17.58 | 14 | 34501 | 2132 | 110552652 |
| Urticaria | 29.06 | 17.58 | 34 | 34481 | 318823 | 110235961 |
| Gastroduodenal ulcer | 28.81 | 17.58 | 11 | 34504 | 960 | 110553824 |
| Dysuria | 28.46 | 17.58 | 60 | 34455 | 60171 | 110494613 |
| Impaired healing | 28.25 | 17.58 | 13 | 34502 | 196704 | 110358080 |
| Pathological fracture | 28.07 | 17.58 | 26 | 34489 | 12006 | 110542778 |
| Radiotherapy | 27.49 | 17.58 | 12 | 34503 | 1476 | 110553308 |
| Swelling | 27.36 | 17.58 | 42 | 34473 | 350999 | 110203785 |
| Bursitis | 27.30 | 17.58 | 4 | 34511 | 129914 | 110424870 |
| Urosepsis | 26.78 | 17.58 | 40 | 34475 | 30635 | 110524149 |
| Sepsis | 25.93 | 17.58 | 183 | 34332 | 327163 | 110227621 |
| Platelet count decreased | 25.91 | 17.58 | 141 | 34374 | 230302 | 110324482 |
| Adrenal insufficiency | 25.83 | 17.58 | 47 | 34468 | 42343 | 110512441 |
| Peri-implantitis | 25.60 | 17.58 | 7 | 34508 | 208 | 110554576 |
| Cough | 25.11 | 17.58 | 68 | 34447 | 461573 | 110093211 |
| Hepatitis fulminant | 24.98 | 17.58 | 21 | 34494 | 8539 | 110546245 |
| Cancer pain | 24.84 | 17.58 | 19 | 34496 | 6753 | 110548031 |
| C-reactive protein increased | 24.82 | 17.58 | 19 | 34496 | 217900 | 110336884 |
| Prostate cancer stage IV | 24.41 | 17.58 | 13 | 34502 | 2475 | 110552309 |
| Groin pain | 24.37 | 17.58 | 27 | 34488 | 15401 | 110539383 |
| Blood chromogranin A increased | 24.28 | 17.58 | 9 | 34506 | 724 | 110554060 |
| Coma | 23.93 | 17.58 | 4 | 34511 | 117865 | 110436919 |
| Allodynia | 23.64 | 17.58 | 12 | 34503 | 2071 | 110552713 |
| Interstitial lung disease | 23.55 | 17.58 | 96 | 34419 | 139238 | 110415546 |
| Arthritis | 22.66 | 17.58 | 12 | 34503 | 167574 | 110387210 |
| Pyrexia | 22.11 | 17.58 | 177 | 34338 | 898088 | 109656696 |
| Blood testosterone increased | 21.73 | 17.58 | 10 | 34505 | 1392 | 110553392 |
| Upper respiratory tract infection | 21.63 | 17.58 | 7 | 34508 | 131321 | 110423463 |
| Retroperitoneal lymphadenopathy | 21.50 | 17.58 | 10 | 34505 | 1426 | 110553358 |
| Thrombocytopenia | 21.50 | 17.58 | 184 | 34331 | 348701 | 110206083 |
| Hip fracture | 21.45 | 17.58 | 39 | 34476 | 35112 | 110519672 |
| Loss of personal independence in daily activities | 21.40 | 17.58 | 10 | 34505 | 150010 | 110404774 |
| Acute myocardial infarction | 21.28 | 17.58 | 66 | 34449 | 83711 | 110471073 |
| Toxic cataract | 21.13 | 17.58 | 4 | 34511 | 20 | 110554764 |
| Soft tissue mass | 20.88 | 17.58 | 10 | 34505 | 1523 | 110553261 |
| Metastases to soft tissue | 20.82 | 17.58 | 8 | 34507 | 711 | 110554073 |
| Gastrointestinal disorder | 20.78 | 17.58 | 27 | 34488 | 241925 | 110312859 |
| Headache | 20.74 | 17.58 | 176 | 34339 | 882201 | 109672583 |
| Nocturia | 20.65 | 17.58 | 26 | 34489 | 16964 | 110537820 |
| Therapeutic product effect incomplete | 20.24 | 17.58 | 24 | 34491 | 223781 | 110331003 |
| Cardiac disorder | 20.22 | 17.58 | 61 | 34454 | 76219 | 110478565 |
| Wound infection | 20.20 | 17.58 | 3 | 34512 | 96462 | 110458322 |
| Pain | 20.05 | 17.58 | 196 | 34319 | 954759 | 109600025 |
| Pyelonephritis acute | 19.62 | 17.58 | 17 | 34498 | 7196 | 110547588 |
| Injection site erythema | 19.56 | 17.58 | 3 | 34512 | 94173 | 110460611 |
| Sleep disorder | 19.40 | 17.58 | 20 | 34495 | 198624 | 110356160 |
| Ischaemic stroke | 19.37 | 17.58 | 41 | 34474 | 41222 | 110513562 |
| Overdose | 19.16 | 17.58 | 27 | 34488 | 233767 | 110321017 |
| Haemorrhage subcutaneous | 19.14 | 17.58 | 15 | 34500 | 5524 | 110549260 |
| Aspartate aminotransferase increased | 18.74 | 17.58 | 99 | 34416 | 159837 | 110394947 |
| Feeling hot | 18.70 | 17.58 | 3 | 34512 | 91103 | 110463681 |
| Ureteral stent insertion | 18.67 | 17.58 | 6 | 34509 | 314 | 110554470 |
| Nasal congestion | 18.54 | 17.58 | 4 | 34511 | 98278 | 110456506 |
| Depressed level of consciousness | 18.47 | 17.58 | 6 | 34509 | 112272 | 110442512 |
| Injury | 18.29 | 17.58 | 17 | 34498 | 177248 | 110377536 |
| Type 2 diabetes mellitus | 18.28 | 17.58 | 17 | 34498 | 177215 | 110377569 |
| Transaminases increased | 18.05 | 17.58 | 52 | 34463 | 63338 | 110491446 |
| Mobility decreased | 17.92 | 17.58 | 29 | 34486 | 237393 | 110317391 |
| Abdominal discomfort | 17.87 | 17.58 | 63 | 34452 | 393795 | 110160989 |
| Long QT syndrome | 17.82 | 17.58 | 16 | 34499 | 7102 | 110547682 |
| Product use issue | 17.63 | 17.58 | 45 | 34470 | 311650 | 110243134 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XK52 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Poly (ADP-ribose) polymerase (PARP) inhibitors |
| ATC | L02BX03 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Other hormone antagonists and related agents |
| ATC | L02BX53 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Other hormone antagonists and related agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D065088 | Steroid Synthesis Inhibitors |
| MeSH PA | D065607 | Cytochrome P-450 Enzyme Inhibitors |
| FDA MoA | N0000182137 | Cytochrome P450 2D6 Inhibitors |
| FDA MoA | N0000182632 | Cytochrome P450 17A1 Inhibitors |
| FDA EPC | N0000182633 | Cytochrome P450 17A1 Inhibitor |
| FDA MoA | N0000187062 | Cytochrome P450 2C8 Inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:50266 | prodrug |
| CHEBI has role | CHEBI:68640 | EC 1.14.99.9 (steroid 17α-monooxygenase) inhibitor |
| CHEBI has role | CHEBI:50113 | androgen |
Related Drugs by ATC class:
L01XK Poly (ADP-ribose) polymerase (PARP) inhibitors 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Malignant tumor of prostate | indication | 399068003 | DOID:10283 |
| Metastatic castration-resistant prostate cancer | indication | 427492003 | |
| Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Hypokalemia | contraindication | 43339004 | |
| Body fluid retention | contraindication | 43498006 | |
| Chronic heart failure | contraindication | 48447003 | |
| Liver function tests abnormal | contraindication | 166603001 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Pregnancy, function | contraindication | 289908002 | |
| Breastfeeding (mother) | contraindication | 413712001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.68 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8071579 | Aug. 12, 2027 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8071579 | Aug. 12, 2027 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8143241 | Aug. 12, 2027 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8143241 | Aug. 12, 2027 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8071579 | Aug. 12, 2027 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8071579 | Aug. 12, 2027 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8143241 | Aug. 12, 2027 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8143241 | Aug. 12, 2027 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8859562 | Aug. 4, 2031 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8859562 | Aug. 4, 2031 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8859562 | Aug. 4, 2031 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 8859562 | Aug. 4, 2031 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 125MG | YONSA | SUN PHARM | N210308 | May 22, 2018 | RX | TABLET | ORAL | 10292990 | May 20, 2034 | USE IN COMBINATION WITH METHYLPREDNISOLONE FOR THE TREATMENT OF PATIENTS WITH PROSTATE CANCER |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11207311 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11207311 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11986468 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11986468 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11986469 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11986469 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11986470 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11992486 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11992486 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 12383543 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 12383543 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11207311 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11207311 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11986468 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11986468 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11986469 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11986469 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11986470 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11992486 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11992486 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 12383543 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 12383543 | July 28, 2037 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11673877 | March 27, 2038 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11673877 | March 27, 2038 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11673877 | March 27, 2038 | A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | 11673877 | March 27, 2038 | A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | Aug. 11, 2026 | NEW PRODUCT |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | Aug. 11, 2026 | NEW PRODUCT |
| 500MG;EQ 100MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | Dec. 12, 2028 | NIRAPARIB/ABIRATERONE ACETATE IN FIXED DOSE COMBINATION WITH PREDNISONE FOR THE TREATMENT OF ADULTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS BRCA2-MUTATED METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER |
| 500MG;EQ 50MG BASE | AKEEGA | JANSSEN BIOTECH | N216793 | Aug. 11, 2023 | RX | TABLET | ORAL | Dec. 12, 2028 | NIRAPARIB/ABIRATERONE ACETATE IN FIXED DOSE COMBINATION WITH PREDNISONE FOR THE TREATMENT OF ADULTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS BRCA2-MUTATED METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Steroid 17-alpha-hydroxylase/17,20 lyase | Enzyme | INHIBITOR | IC50 | 8.54 | CHEMBL | IUPHAR | |||
| Androgen receptor | Nuclear hormone receptor | EC50 | 4.77 | CHEMBL | |||||
| Cytochrome P450 3A4 | Enzyme | IC50 | 5.57 | CHEMBL | |||||
| Cytochrome P450 11B2, mitochondrial | Enzyme | IC50 | 5.76 | CHEMBL | |||||
| Cytochrome P450 21 | Enzyme | IC50 | 6.53 | CHEMBL | |||||
| Cytochrome P450 11B1, mitochondrial | Enzyme | IC50 | 5.79 | CHEMBL | |||||
| Cytochrome P450 17A1 | Enzyme | IC50 | 7.90 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4030721 | VUID |
| N0000182731 | NUI |
| D09701 | KEGG_DRUG |
| 4030720 | VANDF |
| 4030721 | VANDF |
| C2607886 | UMLSCUI |
| AER | PDB_CHEM_ID |
| CHEMBL271227 | ChEMBL_ID |
| CHEMBL254328 | ChEMBL_ID |
| D000069501 | MESH_DESCRIPTOR_UI |
| 9288 | IUPHAR_LIGAND_ID |
| EM5OCB9YJ6 | UNII |
| 9821849 | PUBCHEM_CID |
| DB05812 | DRUGBANK_ID |
| 1100071 | RXNORM |
| 181225 | MMSL |
| 27860 | MMSL |
| 299803 | MMSL |
| d07766 | MMSL |
| 013720 | NDDF |
| 013721 | NDDF |
| 699678007 | SNOMEDCT_US |
| 699679004 | SNOMEDCT_US |
| 767857007 | SNOMEDCT_US |
| C0754011 | UMLSCUI |
| CHEBI:68639 | CHEBI |
| 154229-19-3 | SECONDARY_CAS_RN |
| 132971 | PUBCHEM_CID |
| 6745 | IUPHAR_LIGAND_ID |
| 7375 | INN_ID |
| C089740 | MESH_SUPPLEMENTAL_RECORD_UI |
| G819A456D0 | UNII |
| CHEBI:68642 | CHEBI |
| EM5OCB9YJ6 | INXIGHT DRUGS |
| G819A456D0 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Abiraterone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9597 | TABLET | 250 mg | ORAL | ANDA | 28 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-6920 | TABLET | 250 mg | ORAL | ANDA | 29 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-6921 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 29 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-6948 | TABLET | 250 mg | ORAL | ANDA | 28 sections |
| YONSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 11014-0566 | TABLET | 125 mg | ORAL | Export only | 1 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-963 | TABLET | 250 mg | ORAL | ANDA | 27 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-024 | TABLET | 250 mg | ORAL | ANDA | 27 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-358 | TABLET | 250 mg | ORAL | ANDA | 26 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-468 | TABLET | 500 mg | ORAL | ANDA | 26 sections |
| YONSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47335-401 | TABLET | 125 mg | ORAL | NDA | 27 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50268-032 | TABLET | 250 mg | ORAL | ANDA | 25 sections |
| ABIRATERONE ACETATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-503 | TABLET | 125 mg | ORAL | NDA | 27 sections |
| AKEEGA | HUMAN PRESCRIPTION DRUG LABEL | 2 | 57894-050 | TABLET, FILM COATED | 500 mg | ORAL | NDA | 33 sections |
| AKEEGA | HUMAN PRESCRIPTION DRUG LABEL | 2 | 57894-100 | TABLET, FILM COATED | 500 mg | ORAL | NDA | 33 sections |
| Zytiga | HUMAN PRESCRIPTION DRUG LABEL | 1 | 57894-150 | TABLET | 250 mg | ORAL | NDA | 31 sections |
| Zytiga | HUMAN PRESCRIPTION DRUG LABEL | 1 | 57894-195 | TABLET, FILM COATED | 500 mg | ORAL | NDA | 31 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-1165 | TABLET | 250 mg | ORAL | ANDA | 26 sections |
| ABIRATERONE ACETATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-1754 | TABLET | 500 mg | ORAL | ANDA | 26 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-4327 | TABLET | 250 mg | ORAL | ANDA | 28 sections |
| abiraterone acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-4764 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 32 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-790 | TABLET | 250 mg | ORAL | ANDA | 28 sections |
| Abiraterone acetate | Human Prescription Drug Label | 1 | 64980-418 | TABLET | 250 mg | ORAL | ANDA | 24 sections |
| Abiraterone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68001-489 | TABLET | 250 mg | ORAL | ANDA | 24 sections |
| Abiraterone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68001-673 | TABLET | 500 mg | ORAL | ANDA | 24 sections |
| abiraterone acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68462-135 | TABLET | 250 mg | ORAL | ANDA | 29 sections |
| abiraterone acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68462-882 | TABLET | 500 mg | ORAL | ANDA | 29 sections |
| Abiraterone Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1165 | TABLET | 250 mg | ORAL | ANDA | 26 sections |
| ABIRATERONE ACETATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1754 | TABLET | 500 mg | ORAL | ANDA | 26 sections |
| Abiraterone acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71921-177 | TABLET, FILM COATED | 500 mg | ORAL | ANDA | 32 sections |
| abiraterone acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71921-178 | TABLET | 250 mg | ORAL | ANDA | 32 sections |