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apalutamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| non-steroid antiandrogens | 5278 | 956104-40-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Apalutamide is an Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription. A major metabolite, N-desmethyl apalutamide, is a less potent inhibitor of AR, and exhibited one-third the activity of apalutamide in an in vitro transcriptional reporter assay. Apalutamide administration caused decreased tumor cell proliferation and increased apoptosis leading to decreased tumor volume in mouse xenograft models of prostate cancer.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.24 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.601 | High | 0.81 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.683 | High | 0.81 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 43.954 | 10^-6 cm/s | High | 0.81 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.664 | uL/min/10^6 cells | High | 0.81 |
| dppb | Dog plasma protein binding (% unbound) | 7.300 | % | High | 0.81 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 18.600 | % | High | 0.81 |
| herg | hERG pIC50 | 4.861 | pIC50 | High | 0.81 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.304 | uL/min/10^6 cells | High | 0.81 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.491 | uL/min/mg protein | High | 0.81 |
| hppb | Human plasma protein binding (% unbound) | 5.200 | % | High | 0.81 |
| kinase-safety-class | EIF2AK3,GRK2,PDK1,PDK2,PDK4 | 5 | |||
| kinase-selectivity-class | EIF2AK3,GRK2,PDK1 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.581 | High | 0.81 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 20.324 | High | 0.81 | |
| mppb | Mouse plasma protein binding (% unbound) | 4.330 | High | 0.81 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 7.816 | High | 0.81 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 | |||
| pppb | Pig plasma protein binding (% unbound) | 11.910 | % | High | 0.81 |
| rh-clint | Rat hepatocyte intrinsic clearance | 6.622 | uL/min/10^6 cells | High | 0.81 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 44.550 | % | High | 0.81 |
| rppb | Rat plasma protein binding (% unbound) | 4.040 | % | High | 0.81 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 15.631 | uM | High | 0.81 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 26, 2019 | PMDA | Janssen Pharmaceutical K.K. | |
| Jan. 14, 2019 | EMA | JANSSEN-CILAG INTERNATIONAL N.V. | |
| Feb. 14, 2018 | FDA | JANSSEN BIOTECH |
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Rash | 927.72 | 20.11 | 698 | 11275 | 276256 | 42333106 |
| Hot flush | 599.36 | 20.11 | 228 | 11745 | 22123 | 42587239 |
| Prostatic specific antigen increased | 308.83 | 20.11 | 131 | 11842 | 16794 | 42592568 |
| Death | 237.33 | 20.11 | 450 | 11523 | 470735 | 42138627 |
| Fatigue | 163.22 | 20.11 | 369 | 11604 | 435272 | 42174090 |
| Dermatitis exfoliative generalised | 99.27 | 20.11 | 43 | 11930 | 5781 | 42603581 |
| Hospitalisation | 94.00 | 20.11 | 110 | 11863 | 74220 | 42535142 |
| Pruritus | 88.80 | 20.11 | 176 | 11797 | 188595 | 42420767 |
| Therapy cessation | 72.84 | 20.11 | 54 | 11919 | 20396 | 42588966 |
| Decreased appetite | 61.34 | 20.11 | 154 | 11819 | 192983 | 42416379 |
| Fall | 56.54 | 20.11 | 169 | 11804 | 234351 | 42375011 |
| Interstitial lung disease | 53.30 | 20.11 | 86 | 11887 | 78376 | 42530986 |
| Prostate cancer metastatic | 47.09 | 20.11 | 27 | 11946 | 6602 | 42602760 |
| Hypothyroidism | 44.75 | 20.11 | 50 | 11923 | 32034 | 42577328 |
| Drug reaction with eosinophilia and systemic symptoms | 44.58 | 20.11 | 57 | 11916 | 42018 | 42567344 |
| Blood thyroid stimulating hormone increased | 44.27 | 20.11 | 24 | 11949 | 5268 | 42604094 |
| Metastases to bone | 43.74 | 20.11 | 35 | 11938 | 14774 | 42594588 |
| Taste disorder | 41 | 20.11 | 29 | 11944 | 10178 | 42599184 |
| Rash pruritic | 39.56 | 20.11 | 48 | 11925 | 33555 | 42575807 |
| Agranulocytosis | 38.13 | 20.11 | 45 | 11928 | 30567 | 42578795 |
| Product dose omission issue | 36.89 | 20.11 | 111 | 11862 | 154254 | 42455108 |
| Erythema | 36.84 | 20.11 | 89 | 11884 | 108704 | 42500658 |
| Drug eruption | 35.73 | 20.11 | 38 | 11935 | 23037 | 42586325 |
| Physical deconditioning | 35.32 | 20.11 | 16 | 11957 | 2389 | 42606973 |
| Prostatic specific antigen abnormal | 34.27 | 20.11 | 12 | 11961 | 912 | 42608450 |
| Eczema | 34.26 | 20.11 | 45 | 11928 | 34041 | 42575321 |
| Acute kidney injury | 33.94 | 20.11 | 32 | 11941 | 367305 | 42242057 |
| Treatment noncompliance | 33.71 | 20.11 | 47 | 11926 | 37625 | 42571737 |
| Asthenia | 33.04 | 20.11 | 161 | 11812 | 280632 | 42328730 |
| Toxicity to various agents | 32.33 | 20.11 | 12 | 11961 | 229124 | 42380238 |
| Pollakiuria | 31.25 | 20.11 | 35 | 11938 | 22470 | 42586892 |
| Heat illness | 31.21 | 20.11 | 9 | 11964 | 363 | 42608999 |
| Rash maculo-papular | 30.92 | 20.11 | 45 | 11928 | 37458 | 42571904 |
| Hypertension | 30.74 | 20.11 | 110 | 11863 | 167094 | 42442268 |
| Lichenoid keratosis | 30.52 | 20.11 | 17 | 11956 | 3933 | 42605429 |
| Incorrect dosage administered | 30.31 | 20.11 | 13 | 11960 | 1705 | 42607657 |
| Stevens-Johnson syndrome | 29.96 | 20.11 | 34 | 11939 | 22144 | 42587218 |
| Skin toxicity | 29.58 | 20.11 | 20 | 11953 | 6529 | 42602833 |
| Dry skin | 27.51 | 20.11 | 49 | 11924 | 48289 | 42561073 |
| Erectile dysfunction | 26.77 | 20.11 | 34 | 11939 | 24879 | 42584483 |
| Intestinal transit time decreased | 26.04 | 20.11 | 6 | 11967 | 97 | 42609265 |
| Dizziness | 25.84 | 20.11 | 138 | 11835 | 249116 | 42360246 |
| Toxic epidermal necrolysis | 24.87 | 20.11 | 34 | 11939 | 26716 | 42582646 |
| Blood testosterone increased | 24.85 | 20.11 | 11 | 11962 | 1556 | 42607806 |
| Therapy interrupted | 23.33 | 20.11 | 30 | 11943 | 22220 | 42587142 |
| Rash erythematous | 22.89 | 20.11 | 36 | 11937 | 32055 | 42577307 |
| Condition aggravated | 22.57 | 20.11 | 24 | 11949 | 260730 | 42348632 |
| Hormone-refractory prostate cancer | 22.45 | 20.11 | 9 | 11964 | 995 | 42608367 |
| Pelvic pain | 22.43 | 20.11 | 13 | 11960 | 3241 | 42606121 |
| Prostatic specific antigen decreased | 22.02 | 20.11 | 6 | 11967 | 196 | 42609166 |
| Adverse event | 21.90 | 20.11 | 30 | 11943 | 23610 | 42585752 |
| Restless legs syndrome | 20.78 | 20.11 | 19 | 11954 | 9595 | 42599767 |
| Product size issue | 20.76 | 20.11 | 8 | 11965 | 797 | 42608565 |
| Emergency care | 20.53 | 20.11 | 7 | 11966 | 491 | 42608871 |
| Listless | 20.34 | 20.11 | 10 | 11963 | 1793 | 42607569 |
| Drug ineffective | 20.17 | 20.11 | 100 | 11873 | 630097 | 41979265 |
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 |
|---|---|---|---|---|---|---|
| Hot flush | 461.97 | 22.01 | 180 | 8676 | 65856 | 110514587 |
| Rash | 420.54 | 22.01 | 414 | 8442 | 820550 | 109759893 |
| Prostatic specific antigen increased | 329.84 | 22.01 | 93 | 8763 | 12418 | 110568025 |
| Death | 186.88 | 22.01 | 253 | 8603 | 698616 | 109881827 |
| Dermatitis exfoliative generalised | 113.70 | 22.01 | 40 | 8816 | 10932 | 110569511 |
| Fatigue | 108.64 | 22.01 | 274 | 8582 | 1215684 | 109364759 |
| Interstitial lung disease | 81.21 | 22.01 | 76 | 8780 | 139258 | 110441185 |
| Decreased appetite | 66.88 | 22.01 | 129 | 8727 | 475717 | 110104726 |
| Pruritus | 66.81 | 22.01 | 145 | 8711 | 581415 | 109999028 |
| Erectile dysfunction | 64.71 | 22.01 | 31 | 8825 | 18525 | 110561918 |
| Drug reaction with eosinophilia and systemic symptoms | 58.13 | 22.01 | 50 | 8806 | 82045 | 110498398 |
| Agranulocytosis | 55.02 | 22.01 | 43 | 8813 | 61717 | 110518726 |
| Prostatic specific antigen abnormal | 52.82 | 22.01 | 12 | 8844 | 667 | 110579776 |
| Prostate cancer metastatic | 51.12 | 22.01 | 18 | 8838 | 4925 | 110575518 |
| Eczema | 49.09 | 22.01 | 43 | 8813 | 72250 | 110508193 |
| Physical deconditioning | 48.84 | 22.01 | 16 | 8840 | 3521 | 110576922 |
| Erythema | 45.84 | 22.01 | 83 | 8773 | 291364 | 110289079 |
| Fall | 45.37 | 22.01 | 128 | 8728 | 603354 | 109977089 |
| Lichenoid keratosis | 43.31 | 22.01 | 17 | 8839 | 6285 | 110574158 |
| Drug eruption | 40.67 | 22.01 | 34 | 8822 | 53625 | 110526818 |
| Dry skin | 38.06 | 22.01 | 45 | 8811 | 107608 | 110472835 |
| Pollakiuria | 37.70 | 22.01 | 30 | 8826 | 44165 | 110536278 |
| Metastases to bone | 37.30 | 22.01 | 26 | 8830 | 31346 | 110549097 |
| Heat illness | 35.66 | 22.01 | 9 | 8847 | 783 | 110579660 |
| Treatment noncompliance | 35.34 | 22.01 | 36 | 8820 | 72954 | 110507489 |
| Rash maculo-papular | 33.05 | 22.01 | 35 | 8821 | 74187 | 110506256 |
| Product dose omission issue | 32.11 | 22.01 | 76 | 8780 | 321706 | 110258737 |
| Intestinal transit time decreased | 32.11 | 22.01 | 6 | 8850 | 125 | 110580318 |
| Hospitalisation | 31.02 | 22.01 | 47 | 8809 | 142446 | 110437997 |
| Asthenia | 30.24 | 22.01 | 122 | 8734 | 688877 | 109891566 |
| Drug interaction | 28.15 | 22.01 | 96 | 8760 | 500087 | 110080356 |
| Toxic epidermal necrolysis | 27.50 | 22.01 | 28 | 8828 | 56699 | 110523744 |
| Stevens-Johnson syndrome | 26.17 | 22.01 | 25 | 8831 | 46876 | 110533567 |
| Therapy cessation | 25.20 | 22.01 | 24 | 8832 | 44833 | 110535610 |
| Skin exfoliation | 25.14 | 22.01 | 33 | 8823 | 87618 | 110492825 |
| Incorrect dosage administered | 24.94 | 22.01 | 10 | 8846 | 3908 | 110576535 |
| Product size issue | 24.87 | 22.01 | 7 | 8849 | 924 | 110579519 |
| Blood thyroid stimulating hormone increased | 24.15 | 22.01 | 14 | 8842 | 12287 | 110568156 |
| Rash erythematous | 23.76 | 22.01 | 31 | 8825 | 81801 | 110498642 |
| Listless | 23.57 | 22.01 | 10 | 8846 | 4505 | 110575938 |
| Blood pressure increased | 22.55 | 22.01 | 58 | 8798 | 258315 | 110322128 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L02BB05 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Anti-androgens |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
L02BB Anti-androgens 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Metastasis from malignant tumor of prostate | indication | 314994000 | |
| Malignant tumor of prostate | indication | 399068003 | DOID:10283 |
| Castration-resistant prostate cancer | indication | 427492003 | |
| Pregnancy, function | contraindication | 289908002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.88 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 8802689 | March 27, 2027 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 8802689 | March 27, 2027 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 8802689 | March 27, 2027 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 8802689 | March 27, 2027 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 8445507 | Feb. 14, 2032 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 8445507 | Feb. 14, 2032 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 8445507 | Feb. 14, 2032 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 8445507 | Feb. 14, 2032 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 9481663 | June 4, 2033 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 9481663 | June 4, 2033 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 9481663 | June 4, 2033 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 9481663 | June 4, 2033 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 10849888 | Sept. 23, 2033 | TREATMENT IN COMBINATION WITH ORCHIECTOMY OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 9884054 | Sept. 23, 2033 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | RE49353 | Sept. 23, 2033 | TREATMENT IN COMBINATION WITH A GNRH AGONIST OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | RE50642 | Sept. 23, 2033 | TREATMENT OF NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) BY DAILY ADMINISTRATION OF 180 MG OR 120 MG OF APALUTAMIDE TO PATIENTS RECEIVING A GONADOTROPIN-RELEASING HORMONE (GNRH) ANALOG |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 10849888 | Sept. 23, 2033 | TREATMENT IN COMBINATION WITH ORCHIECTOMY OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 9884054 | Sept. 23, 2033 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | RE49353 | Sept. 23, 2033 | TREATMENT IN COMBINATION WITH A GNRH AGONIST OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | RE50642 | Sept. 23, 2033 | TREATMENT OF NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) BY DAILY ADMINISTRATION OF 180 MG OR 120 MG OF APALUTAMIDE TO PATIENTS RECEIVING A GONADOTROPIN-RELEASING HORMONE (GNRH) ANALOG |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 10702508 | April 30, 2038 | TREATMENT IN COMBINATION WITH ANDROGEN DEPRIVATION THERAPY OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) THAT IMPROVES METASTASIS FREE SURVIVAL |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 10702508 | April 30, 2038 | TREATMENT IN COMBINATION WITH ANDROGEN DEPRIVATION THERAPY OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) THAT IMPROVES METASTASIS FREE SURVIVAL |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 11963952 | Jan. 30, 2040 | TREATMENT OF METASTATIC CASTRATION SENSITIVE PROSTATE CANCER |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 12303497 | Jan. 30, 2040 | DOSAGE MODIFICATION FOLLOWING GRADE 3 TOXICITY OR INTOLERABLE SIDE EFFECT BY DISCONTINUING APALUTAMIDE UNTIL IMPROVEMENT TO ORIGINAL GRADE OR GRADE I IN TREATMENT OF MCSPC PATIENTS THAT INCREASES OVERALL SURVIVAL AND PROGRESSION FREE SURVIVAL |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 12303497 | Jan. 30, 2040 | IMPROVEMENT OF OVERALL SURVIVAL AND PROGRESSION FREE SURVIVAL IN METASTATIC, CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) PATIENTS BY TREATMENT WITH 240 MG ORAL APALUTAMIDE IN COMBINATION WITH ANDROGEN DEPRIVATION THERAPY |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 11963952 | Jan. 30, 2040 | TREATMENT OF METASTATIC CASTRATION SENSITIVE PROSTATE CANCER |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 12303497 | Jan. 30, 2040 | DOSAGE MODIFICATION FOLLOWING GRADE 3 TOXICITY OR INTOLERABLE SIDE EFFECT BY DISCONTINUING APALUTAMIDE UNTIL IMPROVEMENT TO ORIGINAL GRADE OR GRADE I IN TREATMENT OF MCSPC PATIENTS THAT INCREASES OVERALL SURVIVAL AND PROGRESSION FREE SURVIVAL |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 12303497 | Jan. 30, 2040 | IMPROVEMENT OF OVERALL SURVIVAL AND PROGRESSION FREE SURVIVAL IN METASTATIC, CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) PATIENTS BY TREATMENT WITH 240 MG ORAL APALUTAMIDE IN COMBINATION WITH ANDROGEN DEPRIVATION THERAPY |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 11723898 | Jan. 14, 2041 | TREATMENT OF NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) IN A MALE HUMAN WHO HAS SEVERE HEPATIC IMPAIRMENT |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 11723898 | Jan. 14, 2041 | TREATMENT OF NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) IN A MALE HUMAN WHO HAS SEVERE HEPATIC IMPAIRMENT |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Androgen receptor | Nuclear hormone receptor | INHIBITOR | IC50 | 7.80 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Androgen receptor | Transcription factor | ANTAGONIST | Ki | 7.03 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4T36H88UA7 | UNII |
| D11040 | KEGG_DRUG |
| 4037326 | VANDF |
| C4329353 | UMLSCUI |
| CHEBI:755199 | CHEBI |
| CHEMBL3183409 | ChEMBL_ID |
| 24872560 | PUBCHEM_CID |
| DB11901 | DRUGBANK_ID |
| 10118 | INN_ID |
| C572045 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9043 | IUPHAR_LIGAND_ID |
| 766972001 | SNOMEDCT_US |
| 766973006 | SNOMEDCT_US |
| 270303 | MMSL |
| 33762 | MMSL |
| d08741 | MMSL |
| 017466 | NDDF |
| 1999574 | RXNORM |
| 4T36H88UA7 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ERLEADA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59676-600 | TABLET, FILM COATED | 60 mg | ORAL | NDA | 33 sections |
| ERLEADA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59676-604 | TABLET, FILM COATED | 240 mg | ORAL | NDA | 33 sections |