dolutegravir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antivirals 4805 1051375-16-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dolutegravir sodium
  • tivicay
  • dolutegravir
  • GSK 1349572
  • S-349572
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.
  • Molecular weight: 419.39
  • Formula: C20H19F2N3O5
  • CLOGP: 0.08
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 99.18
  • ALOGS: -3.66
  • ROTB: 3
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg O

ADMET properties:

PropertyValueReference
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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.682 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 3.192 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 29.648 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 3.936 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 45.580 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 47.470 % High 1
herg hERG pIC50 4.504 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 3.304 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 4.898 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 31.120 % High 1
kinase-safety-class ACVR2B,EIF2AK3,GRK2,PDK1,PDK2,PDK4 6
kinase-selectivity-class PDK1 1
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 8.035 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 7.852 High 1
mh-clint Mouse hepatocyte intrinsic clearance 21.777 High 1
mppb Mouse plasma protein binding (% unbound) 27.450 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 21.281 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 50.750 % High 1
rat-kpuu-brain Rat brain Kpuu 0.026 % High 1
rh-clint Rat hepatocyte intrinsic clearance 9.016 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 84.960 % High 1
rppb Rat plasma protein binding (% unbound) 27 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 472.063 uM High 1

Approvals:

DateAgencyCompanyOrphan
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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Exposure during pregnancy 1056.21 33.07 605 15493 237805 90374544
Foetal death 759.64 33.07 238 15860 20485 90591864
Foetal exposure during pregnancy 720.53 33.07 275 15823 42700 90569649
Virologic failure 718.26 33.07 146 15952 2078 90610271
Food allergy 711.31 33.07 238 15860 25240 90587109
Abortion spontaneous 649.28 33.07 272 15826 53784 90558565
Immunodeficiency 598.92 33.07 241 15857 42993 90569356
Temperature regulation disorder 595.55 33.07 182 15916 14397 90597952
Maternal exposure during pregnancy 585.68 33.07 494 15604 359569 90252780
Rash erythematous 504.10 33.07 241 15857 64863 90547486
Intentional product misuse 396.26 33.07 228 15870 89376 90522973
Prescribed overdose 372.95 33.07 226 15872 97399 90514950
Upper respiratory tract infection 356.40 33.07 243 15855 128075 90484274
Blood HIV RNA increased 343.75 33.07 67 16031 757 90611592
Hyperhidrosis 340.81 33.07 242 15856 136063 90476286
Pathogen resistance 338.48 33.07 103 15995 8012 90604337
Coeliac disease 326.48 33.07 159 15939 44451 90567898
Fluid retention 295.97 33.07 188 15910 87903 90524446
Thrombocytopenia 290.94 33.07 263 15835 208462 90403887
Congenital umbilical hernia 279.95 33.07 49 16049 287 90612062
Viral mutation identified 278.50 33.07 66 16032 1959 90610390
Stillbirth 270.43 33.07 85 16013 7358 90604991
Overdose 260.50 33.07 219 15879 157490 90454859
Immune reconstitution inflammatory syndrome 229.59 33.07 74 16024 6945 90605404
Asthma 223.77 33.07 244 15854 241916 90370433
Treatment noncompliance 213.53 33.07 126 15972 51601 90560748
Abortion induced 205.81 33.07 78 16020 11810 90600539
Psoriasis 205.28 33.07 186 15912 147568 90464781
Hepatic enzyme increased 188.13 33.07 273 15825 360463 90251886
Product use issue 175.35 33.07 252 15846 329667 90282682
Bursitis 163.98 33.07 156 15942 131498 90480851
Rheumatoid arthritis 146.40 33.07 244 15854 362370 90249979
Hypertension 138.99 33.07 272 15826 457260 90155089
Decreased immune responsiveness 128.68 33.07 51 16047 8697 90603652
Drug resistance 127.77 33.07 75 16023 30374 90581975
Genotype drug resistance test positive 124.56 33.07 26 16072 423 90611926
Premature delivery 118.38 33.07 78 16020 38684 90573665
Hypersensitivity 111.87 33.07 248 15850 454429 90157920
Treatment failure 106.19 33.07 192 15906 303736 90308613
Infusion related reaction 100.98 33.07 226 15872 416554 90195795
Ectopic kidney 98.58 33.07 16 16082 54 90612295
Viral load increased 97.01 33.07 27 16071 1529 90610820
Joint swelling 90.13 33.07 243 15855 503057 90109292
Pre-eclampsia 88.68 33.07 42 16056 11006 90601343
Erythema 87.99 33.07 151 15947 229095 90383254
Live birth 87.67 33.07 88 16010 79019 90533330
Arthralgia 86.11 33.07 17 16081 778505 89833844
Birth mark 83.67 33.07 16 16082 162 90612187
Pyrexia 80.84 33.07 279 15819 660206 89952143
Constipation 79.27 33.07 162 15936 280233 90332116
Renal dysplasia 76.89 33.07 17 16081 367 90611982
Premature baby 75.43 33.07 50 16048 25027 90587322
Hydrops foetalis 74.06 33.07 18 16080 595 90611754
Infection 73.11 33.07 183 15915 361911 90250438
Contraindicated product administered 72.34 33.07 169 15929 319970 90292379
Diarrhoea 71.65 33.07 39 16059 939151 89673198
Back pain 70.10 33.07 166 15932 317009 90295340
Drug interaction 66.92 33.07 150 15948 276303 90336046
Dyspnoea 63.73 33.07 39 16059 880916 89731433
Drug intolerance 63.53 33.07 199 15899 447392 90164957
Swelling 61.96 33.07 3 16095 419055 90193294
Alopecia 60.96 33.07 8 16090 495063 90117286
Abdominal discomfort 60.52 33.07 7 16091 477321 90135028
Malaise 60.28 33.07 15 16083 585971 90026378
Headache 58.89 33.07 305 15793 862441 89749908
Rash 57.51 33.07 286 15812 795814 89816535
Antiviral drug level below therapeutic 57.50 33.07 10 16088 56 90612293
Fall 56.50 33.07 9 16089 481801 90130548
Pain in extremity 56.14 33.07 7 16091 450522 90161827
Atrial septal defect 53.21 33.07 27 16071 8207 90604142
Foetal growth restriction 52.70 33.07 28 16070 9352 90602997
CSF HIV escape syndrome 52.49 33.07 10 16088 99 90612250
Systemic lupus erythematosus 52.21 33.07 3 16095 361893 90250456
Congenital skin dimples 51.62 33.07 10 16088 109 90612240
Single functional kidney 51.53 33.07 12 16086 329 90612020
Dizziness 50.16 33.07 21 16077 589263 90023086
Cystostomy 49.78 33.07 9 16089 65 90612284
Peripheral swelling 47.78 33.07 8 16090 413098 90199251
Vomiting 47.75 33.07 42 16056 788251 89824098
Synovitis 46.75 33.07 3 16095 329749 90282600
Mycoplasma genitalium infection 43.75 33.07 7 16091 21 90612328
Off label use 42.42 33.07 337 15761 1101915 89510434
Immune reconstitution inflammatory syndrome associated tuberculosis 42.04 33.07 11 16087 492 90611857
Oligohydramnios 41.88 33.07 22 16076 7179 90605170
Urticaria 41.11 33.07 4 16094 312730 90299619
Retching 40.92 33.07 31 16067 19128 90593221
Asthenia 40.84 33.07 22 16076 533729 90078620
Macrocephaly 40.24 33.07 9 16089 205 90612144
Premature separation of placenta 39.08 33.07 15 16083 2347 90610002
Renal aplasia 38.92 33.07 10 16088 416 90611933
Low birth weight baby 38.86 33.07 23 16075 9444 90602905
Cough 38.77 33.07 9 16089 368953 90243396
Hepatitis B DNA increased 37.52 33.07 9 16089 281 90612068
Discomfort 37.43 33.07 3 16095 274332 90338017
Endometritis decidual 37.26 33.07 6 16092 19 90612330
Polydactyly 36.50 33.07 9 16089 316 90612033
Hypotension 36.10 33.07 7 16091 325390 90286959
Postpartum haemorrhage 35.31 33.07 14 16084 2387 90609962
Pneumonia 35.10 33.07 37 16061 638022 89974327
Stomatitis 34.85 33.07 4 16094 274694 90337655
Drug level below therapeutic 34.49 33.07 18 16080 5796 90606553
Gestational diabetes 34.01 33.07 22 16076 10560 90601789
Musculoskeletal stiffness 33.71 33.07 6 16092 296526 90315823
Muscle spasms 33.69 33.07 3 16095 251880 90360469
Contusion 33.58 33.07 3 16095 251213 90361136

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Virologic failure 965.91 17.35 230 13505 3764 42603836
Immune reconstitution inflammatory syndrome 865.97 17.35 256 13479 9887 42597713
Blood HIV RNA increased 590.75 17.35 130 13605 1461 42606139
Foetal exposure during pregnancy 520.74 17.35 269 13466 47042 42560558
Viral mutation identified 438.15 17.35 118 13617 3213 42604387
Congenital umbilical hernia 334.69 17.35 63 13672 293 42607307
Pathogen resistance 295.05 17.35 118 13617 11332 42596268
Treatment noncompliance 200.46 17.35 134 13601 37538 42570062
Birth mark 178.13 17.35 33 13702 138 42607462
Viral load increased 160.33 17.35 53 13682 2944 42604656
Drug resistance 149.72 17.35 108 13627 34140 42573460
Syphilis 148.25 17.35 35 13700 547 42607053
CD4 lymphocytes decreased 144.29 17.35 44 13691 1877 42605723
Hepatitis C 100.86 17.35 54 13681 10079 42597521
Drug interaction 98.35 17.35 245 13490 266754 42340846
Drug level decreased 96.04 17.35 52 13683 9925 42597675
Genotype drug resistance test positive 92.23 17.35 28 13707 1176 42606424
Immune reconstitution inflammatory syndrome associated tuberculosis 87.86 17.35 23 13712 558 42607042
Dyslipidaemia 87.64 17.35 48 13687 9370 42598230
Lipodystrophy acquired 83.45 17.35 34 13701 3416 42604184
Mycobacterial infection 77.46 17.35 30 13705 2638 42604962
Congenital skin dimples 54.65 17.35 13 13722 210 42607390
Portal fibrosis 53.78 17.35 14 13721 332 42607268
Osteoporosis 51.76 17.35 41 13694 14865 42592735
Hepatitis A 51.28 17.35 15 13720 553 42607047
Cytomegalovirus chorioretinitis 49.92 17.35 26 13709 4585 42603015
Meningitis cryptococcal 48.90 17.35 23 13712 3260 42604340
Glomerular filtration rate decreased 48.44 17.35 41 13694 16310 42591290
Mycobacterium avium complex infection 47.54 17.35 22 13713 3005 42604595
Faeces pale 46.32 17.35 18 13717 1596 42606004
Hyperferritinaemia 46.08 17.35 14 13721 589 42607011
Acute hepatitis C 44.28 17.35 10 13725 127 42607473
Renal impairment 43.42 17.35 104 13631 110124 42497476
Premature baby 43.38 17.35 45 13690 23108 42584492
Atrial septal defect 41.65 17.35 28 13707 7891 42599709
Nephropathy toxic 41.43 17.35 38 13697 16800 42590800
CSF HIV escape syndrome 40.12 17.35 10 13725 198 42607402
Polydactyly 39.86 17.35 15 13720 1219 42606381
Drug-induced liver injury 39.63 17.35 55 13680 38218 42569382
Human immunodeficiency virus transmission 39.46 17.35 8 13727 58 42607542
Product use in unapproved therapeutic environment 39.25 17.35 11 13724 347 42607253
Trisomy 21 38.10 17.35 12 13723 570 42607030
Scrotal cyst 37.68 17.35 9 13726 148 42607452
Monkeypox 37.67 17.35 11 13724 403 42607197
Hepatotoxicity 36.88 17.35 43 13692 25124 42582476
Lymphadenopathy 36.13 17.35 49 13686 33316 42574284
Suicidal ideation 35.38 17.35 59 13676 48102 42559498
Ocular icterus 35.05 17.35 18 13717 3083 42604517
HIV-associated neurocognitive disorder 35.02 17.35 10 13725 338 42607262
Multiple-drug resistance 34.05 17.35 24 13711 7298 42600302
Disseminated mycobacterium avium complex infection 33.63 17.35 9 13726 238 42607362
Renal failure 33.37 17.35 112 13623 143614 42463986
Chylothorax 33.36 17.35 13 13722 1161 42606439
Blood creatinine increased 33.24 17.35 94 13641 109909 42497691
Peritoneal cyst 33.23 17.35 6 13729 21 42607579
Blood triglycerides abnormal 33.01 17.35 9 13726 256 42607344
Immune recovery uveitis 31.51 17.35 7 13728 82 42607518
Viraemia 31.38 17.35 14 13721 1756 42605844
Fibrous histiocytoma 30.38 17.35 9 13726 347 42607253
Pneumonia 29.69 17.35 57 13678 422092 42185508
Enterovirus infection 28.75 17.35 12 13723 1281 42606319
Anogenital dysplasia 28.26 17.35 7 13728 135 42607465
Osteonecrosis 28.22 17.35 30 13705 15835 42591765
Product dose omission issue 27.97 17.35 111 13624 154254 42453346
Hypotension 26.96 17.35 26 13709 257605 42349995
Eyelid ptosis 26.80 17.35 20 13715 6641 42600959
Fall 26.53 17.35 22 13713 234498 42373102
Progressive multifocal leukoencephalopathy 26.38 17.35 25 13710 11511 42596089
Unmasking of previously unidentified disease 25.97 17.35 11 13724 1218 42606382
Mycobacterium avium complex immune restoration disease 25.34 17.35 5 13730 31 42607569
Talipes 25.33 17.35 13 13722 2223 42605377
Renal tubular disorder 24.96 17.35 17 13718 4892 42602708
Splenomegaly 24.76 17.35 29 13706 17018 42590582
Transplant rejection 24.71 17.35 26 13709 13562 42594038
Floppy eyelid syndrome 24.57 17.35 5 13730 37 42607563
Pelvic kidney 24.51 17.35 6 13729 110 42607490
Hepatitis B 24.46 17.35 19 13716 6692 42600908
Lung transplant rejection 24.23 17.35 10 13725 1037 42606563
Malignant anorectal neoplasm 24.12 17.35 5 13730 41 42607559
Gastroenteritis cryptosporidial 23.88 17.35 7 13728 260 42607340
Blood HIV RNA 23.77 17.35 4 13731 8 42607592
Opportunistic infection 23.73 17.35 12 13723 1989 42605611
Pyroglutamic acidosis 23.40 17.35 9 13726 776 42606824
Acquired immunodeficiency syndrome 23.28 17.35 8 13727 500 42607100
Neural tube defect 23.23 17.35 5 13730 50 42607550
Cerebral toxoplasmosis 23.20 17.35 12 13723 2086 42605514
Abnormal dreams 22.98 17.35 20 13715 8251 42599349
Platelet count decreased 22.95 17.35 8 13727 138573 42469027
Gonorrhoea 22.80 17.35 5 13730 55 42607545
Lymphoedema 22.50 17.35 16 13719 4932 42602668
Hepatitis fulminant 22.47 17.35 16 13719 4943 42602657
Treatment failure 22.41 17.35 57 13678 62567 42545033
Tuberculoid leprosy 21.96 17.35 5 13730 66 42607534
Hepatitis cholestatic 21.91 17.35 21 13714 9803 42597797
Acute HIV infection 21.89 17.35 5 13730 67 42607533
Chronic kidney disease 21.24 17.35 47 13688 47194 42560406
Iodine uptake increased 21.12 17.35 3 13732 0 42607600
Head lag abnormal 21.12 17.35 3 13732 0 42607600
Transient neonatal pustular melanosis 21.12 17.35 3 13732 0 42607600
Ultrasound foetal abnormal 21.12 17.35 3 13732 0 42607600
Hepatic necrosis 20.97 17.35 14 13721 3899 42603701
HIV infection 20.88 17.35 10 13725 1475 42606125
Hepatomegaly 20.46 17.35 22 13713 11763 42595837
Meningomyelocele 20.44 17.35 6 13729 224 42607376
Anogenital warts 20.40 17.35 8 13727 727 42606873
Anal cancer stage 0 20.11 17.35 4 13731 26 42607574
Congenital cerebral cyst 19.85 17.35 4 13731 28 42607572
Product use complaint 19.73 17.35 11 13724 2220 42605380
Calculus urinary 19.28 17.35 10 13725 1747 42605853
Respiratory gas exchange disorder 19.28 17.35 7 13728 514 42607086
Drug abuse 19.24 17.35 5 13730 104766 42502834
Cerebral amyloid angiopathy 19.15 17.35 6 13729 280 42607320
Myopia 19.09 17.35 9 13726 1282 42606318
Chlamydial infection 18.85 17.35 6 13729 295 42607305
Atypical mycobacterial infection 18.60 17.35 9 13726 1357 42606243
Oral candidiasis 18.46 17.35 23 13712 14382 42593218
Cytomegalovirus colitis 18.39 17.35 13 13722 3968 42603632
Hormone-dependent prostate cancer 18.16 17.35 4 13731 45 42607555
Acidosis 18.02 17.35 21 13714 12258 42595342
Febrile neutropenia 17.98 17.35 20 13715 185683 42421917
Cardiac failure congestive 17.95 17.35 3 13732 85599 42522001
Latent syphilis 17.83 17.35 3 13732 6 42607594
Congenital pigmentation disorder 17.83 17.35 3 13732 6 42607594
Toxoplasma serology positive 17.51 17.35 3 13732 7 42607593
Malabsorption 17.51 17.35 11 13724 2762 42604838

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Virologic failure 1300.67 18.58 283 23410 4669 110560937
Immune reconstitution inflammatory syndrome 1078.55 18.58 308 23385 15918 110549688
Blood HIV RNA increased 750.95 18.58 156 23537 2032 110563574
Viral mutation identified 585.95 18.58 145 23548 4274 110561332
Foetal death 580.53 18.58 191 23502 15854 110549752
Exposure during pregnancy 548.18 18.58 377 23316 167047 110398559
Temperature regulation disorder 469.26 18.58 154 23539 12672 110552934
Pathogen resistance 443.32 18.58 160 23533 17512 110548094
Maternal exposure during pregnancy 429.78 18.58 388 23305 254495 110311111
Abortion spontaneous 413.44 18.58 183 23510 34099 110531507
Food allergy 406.35 18.58 155 23538 19793 110545813
Immunodeficiency 357.83 18.58 172 23521 38666 110526940
Treatment noncompliance 354.51 18.58 211 23482 72779 110492827
Coeliac disease 288.75 18.58 154 23539 43033 110522573
Stillbirth 230.41 18.58 69 23624 4195 110561411
Prescribed overdose 210.75 18.58 164 23529 87417 110478189
Rash erythematous 202.93 18.58 156 23537 81676 110483930
Fluid retention 191.70 18.58 160 23533 94147 110471459
Drug resistance 186.53 18.58 128 23565 56246 110509360
Viral load increased 179.46 18.58 54 23639 3336 110562270
Abortion induced 176.61 18.58 66 23627 7953 110557653
Intentional product misuse 171.69 18.58 175 23518 132729 110432877
Genotype drug resistance test positive 165.72 18.58 42 23651 1364 110564242
Drug interaction 164.39 18.58 343 23350 499840 110065766
Syphilis 152.52 18.58 35 23658 739 110564867
Hepatitis C 147.90 18.58 66 23627 12507 110553099
Upper respiratory tract infection 141.40 18.58 157 23536 131171 110434435
Psoriasis 139.91 18.58 161 23532 139832 110425774
Bursitis 132.50 18.58 151 23542 129767 110435839
Foetal exposure during pregnancy 130.43 18.58 52 23641 7453 110558153
Immune reconstitution inflammatory syndrome associated tuberculosis 121.83 18.58 31 23662 1023 110564583
Decreased immune responsiveness 121.29 18.58 53 23640 9553 110556053
Lipodystrophy acquired 117.30 18.58 42 23651 4482 110561124
Hyperhidrosis 114.47 18.58 169 23524 187129 110378477
CD4 lymphocytes decreased 113.95 18.58 37 23656 2937 110562669
Treatment failure 106.32 18.58 203 23490 277031 110288575
Overdose 99.41 18.58 179 23514 233615 110331991
Hepatic enzyme increased 97.06 18.58 213 23480 320679 110244927
CSF HIV escape syndrome 91.41 18.58 20 23673 337 110565269
Thrombocytopenia 88.38 18.58 216 23477 348669 110216937
Dyslipidaemia 79.62 18.58 47 23646 15918 110549688
Drug level decreased 75.61 18.58 48 23645 18500 110547106
Premature delivery 75.00 18.58 58 23635 30574 110535032
Product use issue 74.72 18.58 189 23504 311506 110254100
Asthma 74.34 18.58 165 23528 250126 110315480
Pre-eclampsia 69.72 18.58 35 23658 8615 110556991
Nephropathy toxic 65.04 18.58 51 23642 27427 110538179
Fall 63.44 18.58 25 23668 603457 109962149
Hypertension 63.28 18.58 246 23447 509838 110055768
Mycobacterium avium complex infection 63.25 18.58 29 23664 5848 110559758
Nasopharyngitis 62.75 18.58 6 23687 394355 110171251
Erythema 58.98 18.58 166 23527 291281 110274325
Contraindicated product administered 57.87 18.58 149 23544 248118 110317488
Live birth 56.44 18.58 72 23621 69412 110496194
Antiviral drug level below therapeutic 56.42 18.58 10 23683 51 110565555
Blood triglycerides abnormal 52.06 18.58 14 23679 575 110565031
Osteoporosis 50.84 18.58 77 23616 87075 110478531
Oligohydramnios 50.30 18.58 22 23671 3972 110561634
Oesophageal atresia 50.17 18.58 10 23683 104 110565502
Meningitis cryptococcal 49.69 18.58 23 23670 4739 110560867
Renal failure 48.74 18.58 132 23561 226442 110339164
Rheumatoid arthritis 47.79 18.58 157 23536 299456 110266150
Back pain 47.66 18.58 181 23512 370815 110194791
Synovitis 46.87 18.58 3 23690 274089 110291517
Cystostomy 46.74 18.58 9 23684 77 110565529
Arthropathy 46.73 18.58 4 23689 287518 110278088
Alopecia 45.67 18.58 11 23682 364742 110200864
Portal fibrosis 45.07 18.58 13 23680 692 110564914
Glomerular filtration rate decreased 44.56 18.58 42 23651 28914 110536692
Constipation 43.86 18.58 172 23521 357614 110207992
Monkeypox 43.25 18.58 11 23682 362 110565244
Blood HIV RNA 43.23 18.58 7 23686 18 110565588
Systemic lupus erythematosus 42.85 18.58 3 23690 254335 110311271
Hypotension 42.79 18.58 30 23663 523819 110041787
Hepatitis A 42.75 18.58 14 23679 1141 110564465
Mycoplasma genitalium infection 42.44 18.58 7 23686 21 110565585
Teratogenicity 42.39 18.58 10 23683 239 110565367
Renal dysplasia 42.37 18.58 8 23685 61 110565545
Premature separation of placenta 42.21 18.58 15 23678 1565 110564041
Immunosuppressant drug level increased 42.04 18.58 28 23665 11696 110553910
Mycobacterial infection 41.97 18.58 20 23673 4397 110561209
Pain in extremity 40.98 18.58 27 23666 487091 110078515
Therapeutic product effect decreased 40.82 18.58 3 23690 244313 110321293
Faeces pale 40.69 18.58 18 23675 3339 110562267
Wheezing 40.28 18.58 4 23689 255226 110310380
Disseminated mycobacterium avium complex infection 39.67 18.58 11 23682 507 110565099
Hyperferritinaemia 39.57 18.58 13 23680 1070 110564536
Dyspnoea 39.23 18.58 115 23578 1106757 109458849
Abdominal discomfort 38.67 18.58 18 23675 393840 110171766
Drug intolerance 37.95 18.58 180 23513 406332 110159274
HIV viraemia 37.69 18.58 8 23685 116 110565490
Gestational diabetes 37.49 18.58 22 23671 7367 110558239
HIV-associated neurocognitive disorder 37.49 18.58 10 23683 398 110565208
HIV infection 37.22 18.58 13 23680 1290 110564316
Endometritis decidual 37.18 18.58 6 23687 15 110565591
Malaise 37.17 18.58 54 23639 671765 109893841
Mobility decreased 36.74 18.58 4 23689 237418 110328188
Musculoskeletal stiffness 35.89 18.58 8 23685 279814 110285792
Renal impairment 35.82 18.58 105 23588 188340 110377266
Acute hepatitis C 35.60 18.58 9 23684 289 110565317
Urticaria 35.51 18.58 12 23681 318845 110246761
Arthralgia 35.49 18.58 71 23622 779561 109786045
Sinusitis 35.13 18.58 10 23683 296678 110268928
Fibrous histiocytoma 34.44 18.58 11 23682 828 110564778
Hypersensitivity 34.22 18.58 174 23519 403824 110161782
Pneumonia 34.09 18.58 87 23606 876627 109688979
Pyrexia 33.99 18.58 317 23376 897948 109667658
Suicidal ideation 33.75 18.58 67 23626 93870 110471736
Contusion 33.53 18.58 5 23688 233356 110332250
Peripheral swelling 33.16 18.58 23 23670 404011 110161595
Pericarditis 33.13 18.58 4 23689 219110 110346496
Malaria 32.39 18.58 9 23684 418 110565188
Blister 32.37 18.58 5 23688 227371 110338235
Osteonecrosis 32.31 18.58 38 23655 33703 110531903
Multiple-drug resistance 32.26 18.58 25 23668 13210 110552396
Stomatitis 32.20 18.58 9 23684 270233 110295373
Congenital umbilical hernia 31.75 18.58 5 23688 10 110565596
Retching 31.32 18.58 31 23662 22651 110542955
Immune recovery uveitis 30.72 18.58 7 23686 143 110565463
Single functional kidney 30.40 18.58 8 23685 302 110565304
Headache 30.22 18.58 305 23388 882072 109683534
Eosinophilic pustular folliculitis 30.06 18.58 7 23686 158 110565448
Lymphadenopathy 29.83 18.58 51 23642 63784 110501822
Infusion related reaction 29.41 18.58 160 23533 381002 110184604
Swelling 28.78 18.58 20 23673 351021 110214585
Chlamydial infection 28.63 18.58 9 23684 643 110564963
Total bile acids increased 28.53 18.58 6 23687 83 110565523
Foetal exposure during delivery 28.46 18.58 5 23688 24 110565582
Ocular icterus 28.05 18.58 17 23676 6036 110559570
Cytomegalovirus chorioretinitis 27.94 18.58 18 23675 7110 110558496
Enterovirus infection 27.72 18.58 13 23680 2757 110562849
Injection site pain 27.52 18.58 3 23690 177919 110387687
Lower respiratory tract infection 27.32 18.58 9 23684 243097 110322509
Dry mouth 27.13 18.58 5 23688 199943 110365663
Floppy eyelid syndrome 26.61 18.58 5 23688 37 110565569
Impaired healing 26.52 18.58 5 23688 196712 110368894
Hepatitis B DNA increased 26.24 18.58 9 23684 846 110564760
Hepatotoxicity 26.20 18.58 48 23645 63352 110502254
Cerebral toxoplasmosis 26.17 18.58 13 23680 3129 110562477
Cough 25.61 18.58 37 23656 461604 110104002
Leukopenia 25.54 18.58 80 23613 148711 110416895
Product use in unapproved therapeutic environment 25.37 18.58 7 23686 317 110565289
Hepatitis B 25.29 18.58 19 23674 9593 110556013
Sexual dysfunction 25.01 18.58 18 23675 8512 110557094
Tuberculoma of central nervous system 24.96 18.58 8 23685 609 110564997
Renal tubular disorder 24.86 18.58 17 23676 7412 110558194
Acquired immunodeficiency syndrome 24.67 18.58 7 23686 351 110565255
Renal aplasia 24.66 18.58 6 23687 164 110565442
Gastroenteritis cryptosporidial 24.47 18.58 7 23686 362 110565244
Anogenital dysplasia 24.46 18.58 6 23687 170 110565436
Unmasking of previously unidentified disease 24.28 18.58 12 23681 2856 110562750
Potassium wasting nephropathy 24.16 18.58 6 23687 179 110565427
Drug hypersensitivity 23.99 18.58 173 23520 453917 110111689
Muscle spasms 23.94 18.58 15 23678 278142 110287464
Migraine 23.92 18.58 4 23689 171648 110393958
Drug-induced liver injury 23.86 18.58 68 23625 119999 110445607
Gastrointestinal disorder 23.82 18.58 11 23682 241941 110323665
Anogenital warts 23.74 18.58 9 23684 1127 110564479
Dizziness 23.62 18.58 74 23619 698119 109867487
Foetal growth restriction 23.58 18.58 12 23681 3038 110562568
Pubertal failure 23.57 18.58 4 23689 15 110565591
Premature baby 23.44 18.58 14 23679 4841 110560765
Malignant anorectal neoplasm 23.34 18.58 5 23688 76 110565530
Placenta praevia 22.97 18.58 8 23685 787 110564819
Drug ineffective 22.81 18.58 454 23239 1520086 109045520
Splenomegaly 22.48 18.58 27 23666 24471 110541135
Transplant rejection 22.42 18.58 27 23666 24540 110541066
Iodine uptake increased 22.35 18.58 3 23690 0 110565606
Lung transplant rejection 22.27 18.58 10 23683 1921 110563685
Hyperbilirubinaemia 22.14 18.58 30 23663 30641 110534965
Fibrosis 22.12 18.58 16 23677 7626 110557980
Mycobacterium avium complex immune restoration disease 22.02 18.58 4 23689 24 110565582
Eyelid ptosis 21.79 18.58 20 23673 13307 110552299
Pulmonary tuberculosis 21.71 18.58 17 23676 9122 110556484
Fibromyalgia 21.68 18.58 5 23688 170904 110394702
Generalised anxiety disorder 21.68 18.58 11 23682 2768 110562838
Tuberculoid leprosy 21.50 18.58 5 23688 112 110565494
Premature rupture of membranes 21.43 18.58 13 23680 4624 110560982
C-reactive protein increased 21.31 18.58 10 23683 217909 110347697
Anal cancer stage 0 21.13 18.58 4 23689 31 110565575
Chest pain 21.03 18.58 30 23663 376345 110189261
Cytomegalovirus colitis 20.93 18.58 15 23678 7046 110558560
Injury 20.93 18.58 6 23687 177259 110388347
Coagulopathy 20.87 18.58 34 23659 40877 110524729
Blood pressure increased 20.80 18.58 15 23678 258358 110307248
Joint swelling 20.73 18.58 164 23529 442681 110122925
Oedema peripheral 20.63 18.58 24 23669 328636 110236970
Hepatic necrosis 20.48 18.58 17 23676 9905 110555701
Platelet count decreased 20.43 18.58 12 23681 230431 110335175
Blood creatinine increased 20.05 18.58 85 23608 182804 110382802
Adrenal insufficiency 19.98 18.58 34 23659 42356 110523250
HIV test positive 19.80 18.58 5 23688 160 110565446
Hypoaesthesia 19.66 18.58 23 23670 314200 110251406
Gastrooesophageal reflux disease 19.64 18.58 7 23686 179969 110385637
Therapeutic product effect incomplete 19.35 18.58 12 23681 223793 110341813
Discomfort 19.29 18.58 11 23682 214696 110350910
New onset diabetes after transplantation 19.28 18.58 6 23687 415 110565191
Rash 19.27 18.58 264 23429 820700 109744906
Muscular weakness 19.26 18.58 15 23678 248453 110317153
Arthritis 19.19 18.58 6 23687 167580 110398026
Latent syphilis 19.05 18.58 3 23690 6 110565600
Herpes simplex 18.96 18.58 20 23673 15744 110549862
Atrial fibrillation 18.93 18.58 13 23680 229629 110335977
White matter lesion 18.89 18.58 10 23683 2744 110562862
Diarrhoea 18.89 18.58 155 23538 1139350 109426256
Hepatitis cholestatic 18.87 18.58 21 23672 17545 110548061
Bradycardia 18.85 18.58 5 23688 155512 110410094
Blood cholesterol increased 18.82 18.58 8 23685 184777 110380829
Hyperlactacidaemia 18.79 18.58 15 23678 8271 110557335
Inflammation 18.69 18.58 9 23684 193229 110372377
Hepatomegaly 18.67 18.58 23 23670 21391 110544215
Heart rate increased 18.66 18.58 4 23689 143830 110421776

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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
ATC J05AR29 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 D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D019380 Anti-HIV Agents
MeSH PA D019428 HIV 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
CHEBI has role CHEBI:64946 anti-HIV agent
CHEBI has role CHEBI:67268 HIV-1 integrase inhibitor
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:38068 antimalarial

Related Drugs by ATC class:

J05AJ Integrase inhibitors 3 drugs
cabotegravirelvitegravirraltegravir
J05AR Antivirals for treatment of HIV infections, combinations 19 drugs
abacaviratazanavirbictegravircobicistatdarunavirdoravirineefavirenzelvitegraviremtricitabinelamivudinelopinavirnevirapine show all 19 →

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 8.24 acidic
pKa2 12.47 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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
EQ 50MG BASE;300MG DOVATO VIIV HLTHCARE N211994 April 8, 2019 RX TABLET ORAL April 5, 2027 NEW PATIENT POPULATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA 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 Membrane receptor Ki 7.50 CHEMBL
Integrase Enzyme EC50 8.64 CHEMBL

External reference:

IDSource
DKO1W9H7M1 UNII
D10066 KEGG_DRUG
1051375-19-9 SECONDARY_CAS_RN
4032640 VANDF
C3253985 UMLSCUI
DLU PDB_CHEM_ID
CHEMBL1229211 ChEMBL_ID
54726191 PUBCHEM_CID
DB08930 DRUGBANK_ID
CHEMBL1213165 ChEMBL_ID
D000099226 MESH_DESCRIPTOR_UI
9261 INN_ID
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
CHEBI:76007 CHEBI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 49702-228 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
Juluca HUMAN PRESCRIPTION DRUG LABEL 2 49702-242 TABLET, FILM COATED 50 mg ORAL NDA 27 sections
Juluca HUMAN PRESCRIPTION DRUG LABEL 2 49702-242 TABLET, FILM COATED 50 mg ORAL NDA 27 sections
Dovato HUMAN PRESCRIPTION DRUG LABEL 2 49702-246 TABLET, FILM COATED 50 mg ORAL NDA 28 sections
Dovato HUMAN PRESCRIPTION DRUG LABEL 2 49702-246 TABLET, FILM COATED 50 mg ORAL NDA 28 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 53002-1810 TABLET, FILM COATED 50 mg ORAL NDA 24 sections
Tivicay HUMAN PRESCRIPTION DRUG LABEL 1 53808-1130 TABLET, FILM COATED 50 mg ORAL NDA 25 sections
Tivicay HUMAN PRESCRIPTION DRUG LABEL 1 60760-748 TABLET, FILM COATED 50 mg ORAL NDA 23 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 24 sections