dolutegravir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals | 4805 | 1051375-16-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Dolutegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 0.10 mg/mL | Bocci G, Oprea TI, Benet LZ |
| fu (Fraction unbound in plasma) | 0.00 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 12, 2013 | FDA | VIIV HLTHCARE | |
| March 24, 2014 | PMDA | ViiV Healthcare K.K. | |
| Jan. 16, 2014 | EMA | VIIV HEALTHCARE BV |
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 |
|---|---|---|---|---|---|---|
| Abortion spontaneous | 732.68 | 30.33 | 257 | 7381 | 46938 | 63434446 |
| Exposure during pregnancy | 707.03 | 30.33 | 352 | 7286 | 155195 | 63326189 |
| Foetal exposure during pregnancy | 673.16 | 30.33 | 219 | 7419 | 31743 | 63449641 |
| Virologic failure | 654.13 | 30.33 | 123 | 7515 | 1739 | 63479645 |
| Maternal exposure during pregnancy | 632.12 | 30.33 | 367 | 7271 | 219695 | 63261689 |
| Pathogen resistance | 363.84 | 30.33 | 95 | 7543 | 6303 | 63475081 |
| Blood HIV RNA increased | 357.42 | 30.33 | 64 | 7574 | 675 | 63480709 |
| Foetal death | 325.99 | 30.33 | 98 | 7540 | 10882 | 63470502 |
| Viral mutation identified | 266.36 | 30.33 | 58 | 7580 | 1752 | 63479632 |
| Stillbirth | 256.56 | 30.33 | 73 | 7565 | 6677 | 63474707 |
| Abortion induced | 222.45 | 30.33 | 72 | 7566 | 10170 | 63471214 |
| Treatment noncompliance | 203.03 | 30.33 | 96 | 7542 | 37229 | 63444155 |
| Immune reconstitution inflammatory syndrome | 196.55 | 30.33 | 58 | 7580 | 6026 | 63475358 |
| Congenital umbilical hernia | 190.71 | 30.33 | 33 | 7605 | 280 | 63481104 |
| Live birth | 183.95 | 30.33 | 80 | 7558 | 25550 | 63455834 |
| Drug resistance | 146.56 | 30.33 | 66 | 7572 | 22867 | 63458517 |
| Genotype drug resistance test positive | 135.63 | 30.33 | 26 | 7612 | 407 | 63480977 |
| Premature delivery | 132.00 | 30.33 | 67 | 7571 | 30214 | 63451170 |
| Temperature regulation disorder | 108.68 | 30.33 | 37 | 7601 | 6095 | 63475289 |
| Ectopic kidney | 104.82 | 30.33 | 16 | 7622 | 54 | 63481330 |
| Viral load increased | 100.68 | 30.33 | 25 | 7613 | 1349 | 63480035 |
| Pre-eclampsia | 90.80 | 30.33 | 36 | 7602 | 9097 | 63472287 |
| Birth mark | 89.11 | 30.33 | 16 | 7622 | 171 | 63481213 |
| Food allergy | 86.37 | 30.33 | 37 | 7601 | 11364 | 63470020 |
| Renal dysplasia | 84.60 | 30.33 | 16 | 7622 | 232 | 63481152 |
| Coeliac disease | 82.26 | 30.33 | 37 | 7601 | 12760 | 63468624 |
| Premature baby | 82.03 | 30.33 | 43 | 7595 | 20692 | 63460692 |
| Hydrops foetalis | 75.72 | 30.33 | 17 | 7621 | 591 | 63480793 |
| Immunodeficiency | 66.17 | 30.33 | 37 | 7601 | 20217 | 63461167 |
| Drug interaction | 66.10 | 30.33 | 107 | 7531 | 229024 | 63252360 |
| Foetal growth restriction | 58.81 | 30.33 | 25 | 7613 | 7528 | 63473856 |
| CSF HIV escape syndrome | 56.57 | 30.33 | 10 | 7628 | 97 | 63481287 |
| Oligohydramnios | 56.05 | 30.33 | 23 | 7615 | 6343 | 63475041 |
| Single functional kidney | 55.68 | 30.33 | 12 | 7626 | 344 | 63481040 |
| Antiviral drug level below therapeutic | 55.32 | 30.33 | 9 | 7629 | 50 | 63481334 |
| Congenital skin dimples | 55.26 | 30.33 | 10 | 7628 | 112 | 63481272 |
| Cystostomy | 51.93 | 30.33 | 9 | 7629 | 77 | 63481307 |
| Macrocephaly | 51.33 | 30.33 | 9 | 7629 | 83 | 63481301 |
| Premature separation of placenta | 48.31 | 30.33 | 15 | 7623 | 1846 | 63479538 |
| Atrial septal defect | 47.59 | 30.33 | 21 | 7617 | 6917 | 63474467 |
| Gestational diabetes | 46.82 | 30.33 | 22 | 7616 | 8374 | 63473010 |
| Renal aplasia | 45.64 | 30.33 | 10 | 7628 | 310 | 63481074 |
| Low birth weight baby | 43.87 | 30.33 | 20 | 7618 | 7109 | 63474275 |
| Bursitis | 43.73 | 30.33 | 36 | 7602 | 37005 | 63444379 |
| Prescribed overdose | 42.02 | 30.33 | 34 | 7604 | 34119 | 63447265 |
| Hepatitis B DNA increased | 41.56 | 30.33 | 9 | 7629 | 264 | 63481120 |
| Rash erythematous | 41.40 | 30.33 | 37 | 7601 | 42473 | 63438911 |
| Polydactyly | 40.11 | 30.33 | 9 | 7629 | 312 | 63481072 |
| Mycoplasma genitalium infection | 39.84 | 30.33 | 6 | 7632 | 18 | 63481366 |
| Endometritis decidual | 39.60 | 30.33 | 6 | 7632 | 19 | 63481365 |
| Fluid retention | 37.69 | 30.33 | 41 | 7597 | 59645 | 63421739 |
| Encephalomalacia | 36.26 | 30.33 | 9 | 7629 | 484 | 63480900 |
| Hyperbilirubinaemia | 35.13 | 30.33 | 20 | 7618 | 11294 | 63470090 |
| Potassium wasting nephropathy | 34.76 | 30.33 | 6 | 7632 | 50 | 63481334 |
| Mental disability | 31.99 | 30.33 | 6 | 7632 | 83 | 63481301 |
| Intentional product misuse | 31.93 | 30.33 | 38 | 7600 | 60879 | 63420505 |
| Immunosuppressant drug level increased | 31.53 | 30.33 | 13 | 7625 | 3625 | 63477759 |
| Postpartum haemorrhage | 31.40 | 30.33 | 11 | 7627 | 1970 | 63479414 |
| Osteoporosis | 30.44 | 30.33 | 36 | 7602 | 57302 | 63424082 |
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 |
|---|---|---|---|---|---|---|
| Virologic failure | 915.20 | 18.26 | 216 | 11488 | 3264 | 34941963 |
| Immune reconstitution inflammatory syndrome | 708.93 | 18.26 | 214 | 11490 | 8545 | 34936682 |
| Blood HIV RNA increased | 528.03 | 18.26 | 114 | 11590 | 1116 | 34944111 |
| Viral mutation identified | 390.96 | 18.26 | 106 | 11598 | 2848 | 34942379 |
| Foetal exposure during pregnancy | 299.80 | 18.26 | 176 | 11528 | 37925 | 34907302 |
| Pathogen resistance | 290.77 | 18.26 | 112 | 11592 | 9370 | 34935857 |
| Congenital umbilical hernia | 229.31 | 18.26 | 45 | 11659 | 259 | 34944968 |
| Birth mark | 177.07 | 18.26 | 33 | 11671 | 137 | 34945090 |
| Treatment noncompliance | 167.86 | 18.26 | 109 | 11595 | 27991 | 34917236 |
| Drug resistance | 146.14 | 18.26 | 97 | 11607 | 25830 | 34919397 |
| Viral load increased | 142.75 | 18.26 | 47 | 11657 | 2480 | 34942747 |
| Syphilis | 129.95 | 18.26 | 30 | 11674 | 406 | 34944821 |
| CD4 lymphocytes decreased | 108.96 | 18.26 | 35 | 11669 | 1706 | 34943521 |
| Hepatitis C | 103.29 | 18.26 | 55 | 11649 | 9775 | 34935452 |
| Genotype drug resistance test positive | 88.29 | 18.26 | 27 | 11677 | 1118 | 34944109 |
| Mycobacterial infection | 87.09 | 18.26 | 32 | 11672 | 2342 | 34942885 |
| Drug level decreased | 82.71 | 18.26 | 44 | 11660 | 7802 | 34937425 |
| Drug interaction | 71.74 | 18.26 | 201 | 11503 | 225745 | 34719482 |
| Dyslipidaemia | 70.60 | 18.26 | 39 | 11665 | 7449 | 34937778 |
| Immune reconstitution inflammatory syndrome associated tuberculosis | 58.53 | 18.26 | 16 | 11688 | 442 | 34944785 |
| Meningitis cryptococcal | 54.94 | 18.26 | 23 | 11681 | 2381 | 34942846 |
| Portal fibrosis | 53.78 | 18.26 | 14 | 11690 | 319 | 34944908 |
| Cytomegalovirus chorioretinitis | 52.11 | 18.26 | 25 | 11679 | 3564 | 34941663 |
| Osteoporosis | 51.82 | 18.26 | 39 | 11665 | 12629 | 34932598 |
| Hyperferritinaemia | 49.67 | 18.26 | 14 | 11690 | 434 | 34944793 |
| Hepatitis A | 48.20 | 18.26 | 14 | 11690 | 484 | 34944743 |
| Faeces pale | 48.11 | 18.26 | 18 | 11686 | 1385 | 34943842 |
| Acute hepatitis C | 46.74 | 18.26 | 10 | 11694 | 93 | 34945134 |
| Drug-induced liver injury | 45.30 | 18.26 | 52 | 11652 | 28780 | 34916447 |
| Disseminated mycobacterium avium complex infection | 42.43 | 18.26 | 9 | 11695 | 80 | 34945147 |
| Renal impairment | 41.25 | 18.26 | 95 | 11609 | 94418 | 34850809 |
| Mycobacterium avium complex infection | 41.10 | 18.26 | 19 | 11685 | 2492 | 34942735 |
| Glomerular filtration rate decreased | 40.37 | 18.26 | 34 | 11670 | 12927 | 34932300 |
| Viraemia | 39.26 | 18.26 | 15 | 11689 | 1223 | 34944004 |
| Suicidal ideation | 38.61 | 18.26 | 57 | 11647 | 40331 | 34904896 |
| Chylothorax | 38.05 | 18.26 | 13 | 11691 | 768 | 34944459 |
| Hepatotoxicity | 37.60 | 18.26 | 41 | 11663 | 21444 | 34923783 |
| Nephropathy toxic | 37.12 | 18.26 | 32 | 11672 | 12556 | 34932671 |
| Renal failure | 36.35 | 18.26 | 111 | 11593 | 130446 | 34814781 |
| Fibrous histiocytoma | 36.02 | 18.26 | 9 | 11695 | 173 | 34945054 |
| Lymphadenopathy | 36.00 | 18.26 | 46 | 11658 | 28417 | 34916810 |
| Ocular icterus | 35.80 | 18.26 | 18 | 11686 | 2839 | 34942388 |
| Polydactyly | 32.47 | 18.26 | 13 | 11691 | 1200 | 34944027 |
| Opportunistic infection | 31.75 | 18.26 | 14 | 11690 | 1644 | 34943583 |
| Enterovirus infection | 31.45 | 18.26 | 12 | 11692 | 974 | 34944253 |
| Blood creatinine increased | 30.49 | 18.26 | 85 | 11619 | 94891 | 34850336 |
| Blood HIV RNA | 30.24 | 18.26 | 5 | 11699 | 8 | 34945219 |
| Talipes | 29.76 | 18.26 | 14 | 11690 | 1909 | 34943318 |
| Anogenital warts | 29.33 | 18.26 | 10 | 11694 | 587 | 34944640 |
| Pneumonia | 28.18 | 18.26 | 49 | 11655 | 362578 | 34582649 |
| Blood triglycerides abnormal | 28.17 | 18.26 | 8 | 11696 | 255 | 34944972 |
| Anogenital dysplasia | 28.04 | 18.26 | 7 | 11697 | 134 | 34945093 |
| Multiple-drug resistance | 28.03 | 18.26 | 19 | 11685 | 5220 | 34940007 |
| Lipodystrophy acquired | 27.68 | 18.26 | 16 | 11688 | 3328 | 34941899 |
| Lung transplant rejection | 26.57 | 18.26 | 10 | 11694 | 782 | 34944445 |
| HIV-associated neurocognitive disorder | 26.04 | 18.26 | 8 | 11696 | 336 | 34944891 |
| Abnormal dreams | 25.93 | 18.26 | 21 | 11683 | 7557 | 34937670 |
| CSF HIV escape syndrome | 25.58 | 18.26 | 7 | 11697 | 194 | 34945033 |
| Gastroenteritis cryptosporidial | 25.51 | 18.26 | 7 | 11697 | 196 | 34945031 |
| Premature baby | 25.25 | 18.26 | 32 | 11672 | 19601 | 34925626 |
| Renal tubular disorder | 25.23 | 18.26 | 17 | 11687 | 4626 | 34940601 |
| Hepatitis cholestatic | 25.06 | 18.26 | 21 | 11683 | 7926 | 34937301 |
| Treatment failure | 24.99 | 18.26 | 51 | 11653 | 46646 | 34898581 |
| Splenomegaly | 24.98 | 18.26 | 28 | 11676 | 15089 | 34930138 |
| Malignant anorectal neoplasm | 24.63 | 18.26 | 5 | 11699 | 35 | 34945192 |
| Hepatitis fulminant | 24.36 | 18.26 | 16 | 11688 | 4174 | 34941053 |
| Pelvic kidney | 24.28 | 18.26 | 6 | 11698 | 110 | 34945117 |
| Malabsorption | 24.14 | 18.26 | 13 | 11691 | 2359 | 34942868 |
| Product use complaint | 23.95 | 18.26 | 11 | 11693 | 1421 | 34943806 |
| Fall | 23.57 | 18.26 | 20 | 11684 | 202865 | 34742362 |
| Hypotension | 23.23 | 18.26 | 24 | 11680 | 221625 | 34723602 |
| Neural tube defect | 23.13 | 18.26 | 5 | 11699 | 49 | 34945178 |
| Tuberculoid leprosy | 22.13 | 18.26 | 5 | 11699 | 61 | 34945166 |
| Acute HIV infection | 21.70 | 18.26 | 5 | 11699 | 67 | 34945160 |
| Anal cancer stage 0 | 21.58 | 18.26 | 4 | 11700 | 16 | 34945211 |
| Gonorrhoea | 21.30 | 18.26 | 5 | 11699 | 73 | 34945154 |
| Pharyngeal chlamydia infection | 21.01 | 18.26 | 3 | 11701 | 0 | 34945227 |
| Head lag abnormal | 21.01 | 18.26 | 3 | 11701 | 0 | 34945227 |
| Iodine uptake increased | 21.01 | 18.26 | 3 | 11701 | 0 | 34945227 |
| Transient neonatal pustular melanosis | 21.01 | 18.26 | 3 | 11701 | 0 | 34945227 |
| Hepatic necrosis | 20.88 | 18.26 | 14 | 11690 | 3780 | 34941447 |
| Meningomyelocele | 20.81 | 18.26 | 6 | 11698 | 202 | 34945025 |
| Drug abuse | 20.75 | 18.26 | 4 | 11700 | 99092 | 34846135 |
| Beta 2 microglobulin urine increased | 20.53 | 18.26 | 5 | 11699 | 86 | 34945141 |
| Transplant rejection | 20.38 | 18.26 | 21 | 11683 | 10290 | 34934937 |
| Tinea pedis | 20.36 | 18.26 | 10 | 11694 | 1499 | 34943728 |
| Hepatomegaly | 20.24 | 18.26 | 21 | 11683 | 10375 | 34934852 |
| Myopia | 19.86 | 18.26 | 9 | 11695 | 1127 | 34944100 |
| Hepatic function abnormal | 19.77 | 18.26 | 45 | 11659 | 44318 | 34900909 |
| Chronic kidney disease | 19.71 | 18.26 | 43 | 11661 | 41167 | 34904060 |
| Immune recovery uveitis | 19.34 | 18.26 | 4 | 11700 | 31 | 34945196 |
| Platelet count decreased | 19.24 | 18.26 | 8 | 11696 | 119709 | 34825518 |
| Acquired immunodeficiency syndrome | 19.06 | 18.26 | 7 | 11697 | 511 | 34944716 |
| Cell death | 18.78 | 18.26 | 11 | 11693 | 2346 | 34942881 |
| Hyperlactacidaemia | 18.72 | 18.26 | 12 | 11692 | 3004 | 34942223 |
| Toxoplasma serology positive | 18.47 | 18.26 | 3 | 11701 | 4 | 34945223 |
| HIV infection | 18.45 | 18.26 | 9 | 11695 | 1330 | 34943897 |
| Neurosyphilis | 18.43 | 18.26 | 4 | 11700 | 40 | 34945187 |
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 |
|---|---|---|---|---|---|---|
| Virologic failure | 1198.86 | 17.67 | 254 | 15777 | 3937 | 79724420 |
| Immune reconstitution inflammatory syndrome | 834.30 | 17.67 | 240 | 15791 | 13601 | 79714756 |
| Blood HIV RNA increased | 682.58 | 17.67 | 138 | 15893 | 1670 | 79726687 |
| Viral mutation identified | 526.87 | 17.67 | 128 | 15903 | 3730 | 79724627 |
| Exposure during pregnancy | 432.47 | 17.67 | 263 | 15768 | 100869 | 79627488 |
| Pathogen resistance | 422.68 | 17.67 | 144 | 15887 | 14198 | 79714159 |
| Maternal exposure during pregnancy | 402.09 | 17.67 | 281 | 15750 | 136257 | 79592100 |
| Abortion spontaneous | 397.14 | 17.67 | 167 | 15864 | 29340 | 79699017 |
| Treatment noncompliance | 284.17 | 17.67 | 159 | 15872 | 52109 | 79676248 |
| Foetal death | 199.29 | 17.67 | 71 | 15960 | 7973 | 79720384 |
| Stillbirth | 196.01 | 17.67 | 59 | 15972 | 3896 | 79724461 |
| Abortion induced | 177.07 | 17.67 | 63 | 15968 | 7046 | 79721311 |
| Viral load increased | 176.88 | 17.67 | 51 | 15980 | 2897 | 79725460 |
| Genotype drug resistance test positive | 176.49 | 17.67 | 43 | 15988 | 1265 | 79727092 |
| Drug resistance | 170.44 | 17.67 | 106 | 15925 | 42107 | 79686250 |
| Syphilis | 143.64 | 17.67 | 31 | 16000 | 523 | 79727834 |
| Hepatitis C | 142.18 | 17.67 | 62 | 15969 | 11863 | 79716494 |
| Drug interaction | 131.54 | 17.67 | 270 | 15761 | 414913 | 79313444 |
| Live birth | 121.15 | 17.67 | 64 | 15967 | 18680 | 79709677 |
| Foetal exposure during pregnancy | 106.25 | 17.67 | 41 | 15990 | 5749 | 79722608 |
| Osteoporosis | 76.97 | 17.67 | 73 | 15958 | 54039 | 79674318 |
| CSF HIV escape syndrome | 76.51 | 17.67 | 17 | 16014 | 330 | 79728027 |
| CD4 lymphocytes decreased | 75.79 | 17.67 | 26 | 16005 | 2608 | 79725749 |
| Immune reconstitution inflammatory syndrome associated tuberculosis | 75.76 | 17.67 | 20 | 16011 | 816 | 79727541 |
| Temperature regulation disorder | 74.91 | 17.67 | 32 | 15999 | 5821 | 79722536 |
| Drug level decreased | 70.61 | 17.67 | 41 | 15990 | 14361 | 79713996 |
| Dyslipidaemia | 67.55 | 17.67 | 37 | 15994 | 11596 | 79716761 |
| Nephropathy toxic | 66.91 | 17.67 | 45 | 15986 | 20374 | 79707983 |
| Pre-eclampsia | 66.13 | 17.67 | 31 | 16000 | 7010 | 79721347 |
| Premature delivery | 65.82 | 17.67 | 47 | 15984 | 23420 | 79704937 |
| Immunodeficiency | 59.68 | 17.67 | 43 | 15988 | 21725 | 79706632 |
| Oligohydramnios | 58.49 | 17.67 | 23 | 16008 | 3389 | 79724968 |
| Coeliac disease | 57.47 | 17.67 | 33 | 15998 | 11318 | 79717039 |
| Food allergy | 56.23 | 17.67 | 32 | 15999 | 10792 | 79717565 |
| Renal failure | 54.56 | 17.67 | 123 | 15908 | 200845 | 79527512 |
| Meningitis cryptococcal | 54.42 | 17.67 | 22 | 16009 | 3484 | 79724873 |
| Antiviral drug level below therapeutic | 52.19 | 17.67 | 9 | 16022 | 41 | 79728316 |
| Oesophageal atresia | 51.44 | 17.67 | 10 | 16021 | 97 | 79728260 |
| Drug-induced liver injury | 49.96 | 17.67 | 64 | 15967 | 66053 | 79662304 |
| Blood HIV RNA | 49.80 | 17.67 | 8 | 16023 | 21 | 79728336 |
| Portal fibrosis | 47.52 | 17.67 | 13 | 16018 | 608 | 79727749 |
| Mycobacterial infection | 46.76 | 17.67 | 20 | 16011 | 3648 | 79724709 |
| Lipodystrophy acquired | 46.76 | 17.67 | 21 | 16010 | 4304 | 79724053 |
| Cystostomy | 46.71 | 17.67 | 9 | 16022 | 83 | 79728274 |
| Premature separation of placenta | 46.64 | 17.67 | 15 | 16016 | 1231 | 79727126 |
| Hyperferritinaemia | 45.29 | 17.67 | 13 | 16018 | 726 | 79727631 |
| Fall | 43.34 | 17.67 | 22 | 16009 | 487607 | 79240750 |
| Teratogenicity | 42.95 | 17.67 | 10 | 16021 | 241 | 79728116 |
| Suicidal ideation | 42.81 | 17.67 | 64 | 15967 | 76276 | 79652081 |
| Gestational diabetes | 42.11 | 17.67 | 22 | 16009 | 6271 | 79722086 |
| Hepatitis A | 41.92 | 17.67 | 13 | 16018 | 948 | 79727409 |
| Glomerular filtration rate decreased | 40.90 | 17.67 | 35 | 15996 | 22667 | 79705690 |
| Faeces pale | 40.65 | 17.67 | 17 | 16014 | 2933 | 79725424 |
| Disseminated mycobacterium avium complex infection | 39.01 | 17.67 | 9 | 16022 | 208 | 79728149 |
| Acute hepatitis C | 38.69 | 17.67 | 9 | 16022 | 216 | 79728141 |
| Endometritis decidual | 37.56 | 17.67 | 6 | 16025 | 15 | 79728342 |
| Renal dysplasia | 37.33 | 17.67 | 7 | 16024 | 55 | 79728302 |
| Nasopharyngitis | 36.92 | 17.67 | 4 | 16027 | 253877 | 79474480 |
| Fibrous histiocytoma | 36.80 | 17.67 | 11 | 16020 | 708 | 79727649 |
| Mycoplasma genitalium infection | 36.76 | 17.67 | 6 | 16025 | 18 | 79728339 |
| Mycobacterium avium complex infection | 36.37 | 17.67 | 18 | 16013 | 4582 | 79723775 |
| Renal impairment | 35.69 | 17.67 | 90 | 15941 | 157693 | 79570664 |
| Hepatotoxicity | 34.61 | 17.67 | 47 | 15984 | 51305 | 79677052 |
| Anogenital warts | 33.97 | 17.67 | 11 | 16020 | 923 | 79727434 |
| Lymphadenopathy | 33.28 | 17.67 | 47 | 15984 | 53200 | 79675157 |
| Malaria | 33.07 | 17.67 | 9 | 16022 | 413 | 79727944 |
| Enterovirus infection | 32.94 | 17.67 | 13 | 16018 | 1934 | 79726423 |
| Immunosuppressant drug level increased | 32.25 | 17.67 | 21 | 16010 | 9006 | 79719351 |
| HIV infection | 31.94 | 17.67 | 11 | 16020 | 1116 | 79727241 |
| Hypotension | 30.79 | 17.67 | 26 | 16005 | 440291 | 79288066 |
| Ocular icterus | 30.57 | 17.67 | 17 | 16014 | 5483 | 79722874 |
| Multiple-drug resistance | 30.27 | 17.67 | 20 | 16011 | 8788 | 79719569 |
| HIV-associated neurocognitive disorder | 29.90 | 17.67 | 8 | 16023 | 344 | 79728013 |
| Total bile acids increased | 28.40 | 17.67 | 6 | 16025 | 91 | 79728266 |
| Renal tubular disorder | 27.97 | 17.67 | 17 | 16014 | 6469 | 79721888 |
| Blood creatinine increased | 27.60 | 17.67 | 81 | 15950 | 154976 | 79573381 |
| Sexual dysfunction | 27.59 | 17.67 | 18 | 16013 | 7745 | 79720612 |
| Blood triglycerides abnormal | 27.23 | 17.67 | 8 | 16023 | 485 | 79727872 |
| Hepatitis B DNA increased | 27.22 | 17.67 | 9 | 16022 | 806 | 79727551 |
| Eosinophilic pustular folliculitis | 27.02 | 17.67 | 6 | 16025 | 116 | 79728241 |
| Gastroenteritis cryptosporidial | 26.53 | 17.67 | 7 | 16024 | 285 | 79728072 |
| Single functional kidney | 26.51 | 17.67 | 7 | 16024 | 286 | 79728071 |
| Anogenital dysplasia | 26.33 | 17.67 | 6 | 16025 | 131 | 79728226 |
| Alopecia | 26.30 | 17.67 | 7 | 16024 | 231348 | 79497009 |
| Pneumonia | 26.06 | 17.67 | 59 | 15972 | 660187 | 79068170 |
| Hepatic function abnormal | 25.96 | 17.67 | 50 | 15981 | 73057 | 79655300 |
| Splenomegaly | 25.76 | 17.67 | 26 | 16005 | 20728 | 79707629 |
| Foetal growth restriction | 25.19 | 17.67 | 11 | 16020 | 2108 | 79726249 |
| Lung transplant rejection | 25.12 | 17.67 | 10 | 16021 | 1521 | 79726836 |
| Potassium wasting nephropathy | 25.04 | 17.67 | 6 | 16025 | 164 | 79728193 |
| New onset diabetes after transplantation | 25.04 | 17.67 | 6 | 16025 | 164 | 79728193 |
| Congenital umbilical hernia | 25.04 | 17.67 | 4 | 16027 | 10 | 79728347 |
| Hyperlactacidaemia | 24.99 | 17.67 | 15 | 16016 | 5580 | 79722777 |
| Generalised anxiety disorder | 24.81 | 17.67 | 11 | 16020 | 2186 | 79726171 |
| Diabetes mellitus | 24.69 | 17.67 | 51 | 15980 | 78339 | 79650018 |
| Prescribed overdose | 24.51 | 17.67 | 34 | 15997 | 37849 | 79690508 |
| Coagulopathy | 24.32 | 17.67 | 33 | 15998 | 35973 | 79692384 |
| Hepatitis cholestatic | 24.22 | 17.67 | 21 | 16010 | 13831 | 79714526 |
| Placenta praevia | 23.87 | 17.67 | 8 | 16023 | 747 | 79727610 |
| Hyperbilirubinaemia | 23.86 | 17.67 | 27 | 16004 | 24491 | 79703866 |
| Malignant anorectal neoplasm | 23.84 | 17.67 | 5 | 16026 | 73 | 79728284 |
| Pubertal failure | 23.82 | 17.67 | 4 | 16027 | 15 | 79728342 |
| Premature rupture of membranes | 23.78 | 17.67 | 13 | 16018 | 4056 | 79724301 |
| Pain in extremity | 23.71 | 17.67 | 23 | 16008 | 364515 | 79363842 |
| Osteonecrosis | 23.32 | 17.67 | 30 | 16001 | 31065 | 79697292 |
| Fibrosis | 23.11 | 17.67 | 14 | 16017 | 5295 | 79723062 |
| Bursitis | 22.93 | 17.67 | 32 | 15999 | 35812 | 79692545 |
| Hepatic necrosis | 22.73 | 17.67 | 17 | 16014 | 9083 | 79719274 |
| Anal cancer stage 0 | 22.72 | 17.67 | 4 | 16027 | 21 | 79728336 |
| Pulmonary tuberculosis | 22.62 | 17.67 | 16 | 16015 | 7849 | 79720508 |
| Iodine uptake increased | 22.54 | 17.67 | 3 | 16028 | 0 | 79728357 |
| Pharyngeal chlamydia infection | 22.54 | 17.67 | 3 | 16028 | 0 | 79728357 |
| White matter lesion | 22.44 | 17.67 | 10 | 16021 | 2012 | 79726345 |
| Tuberculoid leprosy | 22.04 | 17.67 | 5 | 16026 | 107 | 79728250 |
| Chlamydial infection | 22.04 | 17.67 | 7 | 16024 | 552 | 79727805 |
| Premature baby | 21.88 | 17.67 | 12 | 16019 | 3768 | 79724589 |
| Tuberculoma of central nervous system | 21.70 | 17.67 | 7 | 16024 | 580 | 79727777 |
| Acquired immunodeficiency syndrome | 21.53 | 17.67 | 6 | 16025 | 301 | 79728056 |
| Persecutory delusion | 21.51 | 17.67 | 13 | 16018 | 4896 | 79723461 |
| Hepatitis fulminant | 21.41 | 17.67 | 15 | 16016 | 7247 | 79721110 |
| Immune recovery uveitis | 21.38 | 17.67 | 4 | 16027 | 31 | 79728326 |
| HIV test positive | 21.15 | 17.67 | 5 | 16026 | 129 | 79728228 |
| Renal aplasia | 21 | 17.67 | 5 | 16026 | 133 | 79728224 |
| Dyspnoea | 20.92 | 17.67 | 95 | 15936 | 856930 | 78871427 |
| Hyperthyroidism | 20.84 | 17.67 | 24 | 16007 | 22185 | 79706172 |
| Hepatic enzyme increased | 20.68 | 17.67 | 82 | 15949 | 182528 | 79545829 |
| Treatment failure | 20.48 | 17.67 | 78 | 15953 | 170408 | 79557949 |
| Hepatomegaly | 20.47 | 17.67 | 22 | 16009 | 18852 | 79709505 |
| Cholestasis | 20.19 | 17.67 | 37 | 15994 | 52072 | 79676285 |
| Cytomegalovirus chorioretinitis | 20.17 | 17.67 | 13 | 16018 | 5477 | 79722880 |
| Transplant rejection | 19.94 | 17.67 | 22 | 16009 | 19415 | 79708942 |
| Pain | 19.67 | 17.67 | 74 | 15957 | 703728 | 79024629 |
| Myelopathy | 19.61 | 17.67 | 12 | 16019 | 4621 | 79723736 |
| Disseminated sporotrichosis | 19.58 | 17.67 | 4 | 16027 | 51 | 79728306 |
| Myopia | 19.57 | 17.67 | 9 | 16022 | 1947 | 79726410 |
| Abnormal dreams | 19.35 | 17.67 | 17 | 16014 | 11395 | 79716962 |
| Musculoskeletal stiffness | 18.60 | 17.67 | 6 | 16025 | 175002 | 79553355 |
| Infected vasculitis | 18.38 | 17.67 | 3 | 16028 | 9 | 79728348 |
| Gonorrhoea | 18.38 | 17.67 | 5 | 16026 | 229 | 79728128 |
| Oral candidiasis | 18.28 | 17.67 | 26 | 16005 | 29602 | 79698755 |
| Foetal exposure during delivery | 17.92 | 17.67 | 3 | 16028 | 11 | 79728346 |
| Contusion | 17.88 | 17.67 | 4 | 16027 | 148772 | 79579585 |
| Arteriovenous graft site pseudoaneurysm | 17.71 | 17.67 | 3 | 16028 | 12 | 79728345 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AJ03 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Integrase inhibitors |
| ATC | J05AR13 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations |
| ATC | J05AR21 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations |
| ATC | J05AR25 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations |
| ATC | J05AR27 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations |
| FDA MoA | N0000000127 | HIV Integrase Inhibitors |
| MeSH PA | D019380 | Anti-HIV Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D044966 | Anti-Retroviral Agents |
| MeSH PA | D000998 | Antiviral Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D019428 | HIV Integrase Inhibitors |
| MeSH PA | D019429 | Integrase Inhibitors |
| FDA EPC | N0000175887 | Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor |
| FDA MoA | N0000187061 | Organic Cation Transporter 2 Inhibitors |
| FDA MoA | N0000191423 | Multidrug and Toxin Extrusion Transporter 1 Inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Human immunodeficiency virus infection | indication | 86406008 | DOID:526 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.24 | acidic |
| pKa2 | 12.47 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 50MG BASE;EQ 25MG BASE | JULUCA | VIIV HLTHCARE | N210192 | Nov. 21, 2017 | RX | TABLET | ORAL | 7125879 | April 21, 2025 | TREATMENT OF HIV INFECTION |
| EQ 50MG BASE;EQ 25MG BASE | JULUCA | VIIV HLTHCARE | N210192 | Nov. 21, 2017 | RX | TABLET | ORAL | 10426780 | Jan. 24, 2031 | TREATMENT OF HIV INFECTION |
| EQ 50MG BASE;300MG | DOVATO | VIIV HLTHCARE | N211994 | April 8, 2019 | RX | TABLET | ORAL | 11234985 | Jan. 24, 2031 | TREATMENT OF HIV INFECTION |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 50MG BASE;300MG | DOVATO | VIIV HLTHCARE | N211994 | April 8, 2019 | RX | TABLET | ORAL | Aug. 6, 2023 | TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY SUPRESSED (HIV-1 RNA LESS THAN 50 COPIES PER ML) ON A STABLE ANTIRETROVIRAL REGIMEN WITH NO HISTORY OF TREATMENT FAILURE |
| EQ 600MG BASE;EQ 50MG BASE;300MG | TRIUMEQ | VIIV HLTHCARE | N205551 | Aug. 22, 2014 | RX | TABLET | ORAL | June 15, 2026 | INFORMATION ADDED TO THE LABELING REGARDING THE RESULT OF STUDY 205860 |
| EQ 60MG BASE;EQ 5MG BASE;30MG | TRIUMEQ PD | VIIV HLTHCARE | N215413 | March 30, 2022 | RX | TABLET, FOR SUSPENSION | ORAL | June 15, 2026 | NEW PATIENT POPULATION |
| EQ 600MG BASE;EQ 50MG BASE;300MG | TRIUMEQ | VIIV HLTHCARE | N205551 | Aug. 22, 2014 | RX | TABLET | ORAL | Dec. 15, 2026 | PEDIATRIC EXCLUSIVITY |
| EQ 60MG BASE;EQ 5MG BASE;30MG | TRIUMEQ PD | VIIV HLTHCARE | N215413 | March 30, 2022 | RX | TABLET, FOR SUSPENSION | ORAL | Dec. 15, 2026 | PEDIATRIC EXCLUSIVITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Transmembrane protein 97 | Enzyme | Ki | 7.75 | CHEMBL | |||||
| Integrase | Enzyme | INHIBITOR | IC50 | 8.13 | SCIENTIFIC LITERATURE | CHEMBL | |||
| Sigma non-opioid intracellular receptor 1 | Membrane other | Ki | 7.15 | CHEMBL | |||||
| Vesicular acetylcholine transporter | Transporter | Ki | 5.34 | CHEMBL | |||||
| Integrase | Enzyme | IC50 | 8.57 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 6.66 | CHEMBL | |||||
| Sigma intracellular receptor 2 | Unclassified | Ki | 7.50 | CHEMBL | |||||
| Integrase | Unclassified | EC50 | 8.64 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| DKO1W9H7M1 | UNII |
| D10066 | KEGG_DRUG |
| 1051375-19-9 | SECONDARY_CAS_RN |
| 4032640 | VANDF |
| C3253985 | UMLSCUI |
| CHEBI:76007 | CHEBI |
| DLU | PDB_CHEM_ID |
| CHEMBL1229211 | ChEMBL_ID |
| 54726191 | PUBCHEM_CID |
| DB08930 | DRUGBANK_ID |
| CHEMBL1213165 | ChEMBL_ID |
| 9261 | INN_ID |
| C562325 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7365 | IUPHAR_LIGAND_ID |
| 1433867 | RXNORM |
| 205031 | MMSL |
| 29613 | MMSL |
| 30505 | MMSL |
| d08117 | MMSL |
| 015174 | NDDF |
| 015175 | NDDF |
| 713464000 | SNOMEDCT_US |
| 713465004 | SNOMEDCT_US |
| 714767001 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-226 | TABLET, FILM COATED | 10 mg | ORAL | NDA | 25 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-226 | TABLET, FILM COATED | 10 mg | ORAL | NDA | 25 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-226 | TABLET, FILM COATED | 10 mg | ORAL | NDA | 25 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-227 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 25 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-227 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 25 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-227 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 25 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-228 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 25 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-228 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 25 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-228 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 25 sections |
| Triumeq | HUMAN PRESCRIPTION DRUG LABEL | 3 | 49702-231 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 27 sections |
| Triumeq | HUMAN PRESCRIPTION DRUG LABEL | 3 | 49702-231 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 27 sections |
| Triumeq | HUMAN PRESCRIPTION DRUG LABEL | 3 | 49702-231 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 27 sections |
| Triumeq | HUMAN PRESCRIPTION DRUG LABEL | 3 | 49702-231 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 27 sections |
| Juluca | HUMAN PRESCRIPTION DRUG LABEL | 2 | 49702-242 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 28 sections |
| Juluca | HUMAN PRESCRIPTION DRUG LABEL | 2 | 49702-242 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 28 sections |
| Juluca | HUMAN PRESCRIPTION DRUG LABEL | 2 | 49702-242 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 28 sections |
| Juluca | HUMAN PRESCRIPTION DRUG LABEL | 2 | 49702-242 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 28 sections |
| Dovato | HUMAN PRESCRIPTION DRUG LABEL | 2 | 49702-246 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 29 sections |
| Dovato | HUMAN PRESCRIPTION DRUG LABEL | 2 | 49702-246 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 29 sections |
| Dovato | HUMAN PRESCRIPTION DRUG LABEL | 2 | 49702-246 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 29 sections |
| Dovato | HUMAN PRESCRIPTION DRUG LABEL | 2 | 49702-246 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 29 sections |
| Tivicay PD | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-255 | TABLET, FOR SUSPENSION | 5 mg | ORAL | NDA | 25 sections |
| Tivicay PD | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-255 | TABLET, FOR SUSPENSION | 5 mg | ORAL | NDA | 25 sections |
| Tivicay PD | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-255 | TABLET, FOR SUSPENSION | 5 mg | ORAL | NDA | 25 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-1130 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 25 sections |
| Dolutegravir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65015-353 | TABLET, FOR SUSPENSION | 10 mg | ORAL | Export only | 1 sections |
| Dolutegravir | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65015-353 | TABLET, FOR SUSPENSION | 10 mg | ORAL | Export only | 1 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67296-1818 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 25 sections |
| Tivicay | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-1487 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 25 sections |