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

Stem definitionDrug idCAS RN
antivirals carbocyclic nucleosides 34 136470-78-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • 1592U89
  • abacavir
  • abacavir sulfate
  • ziagen
  • abacavir succinate
a carbocyclic nucleoside with potent selective anti-HIV activity; structure given in first source
  • Molecular weight: 286.34
  • Formula: C14H18N6O
  • CLOGP: 0.81
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 101.88
  • ALOGS: -2.37
  • ROTB: 4
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.60 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 77 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1.20 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 29.93 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 83 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.84 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 13 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.50 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.168 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 9.550 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 13.274 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 3.281 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 76.560 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 83.650 % High 1
herg hERG pIC50 4.159 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.172 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.184 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 67.480 % High 1
kinase-safety-class ACVR2B,ALK,AURKA,AURKB,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK8,CDK9,CLK1,CLK2,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,DYRK2,EGFR,EIF2AK3,ERBB2,FLT3,GAK,GRK2,GSK3B,HASPIN,IRAK1,IRAK3,IRAK4,ITK,JAK1,KDR,LCK,MAP3K1,MAP3K10,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK15,MAPK3,MAPK7,MARK4,MELK,MET,NTRK1,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PRKCD,PRKDC,SIK2,SIK3,SRC,STK33,SYK,TTK,TYRO3,ULK1 77
kinase-selectivity-class AXL,CAMK2B,CAMK2D,CDK1,CDK16,CDK2,CDK3,CDK4,CDK6,CDK7,CDK8,CDK9,CLK2,CLK4,DYRK1A,DYRK1B,EGFR,EIF2AK3,HASPIN,IRAK1,IRAK3,IRAK4,MAP3K21,MAP4K1,NTRK1,PDK1,PIK3CD,TTK 28
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 7.656 High 1
mh-clint Mouse hepatocyte intrinsic clearance 18.535 High 1
mppb Mouse plasma protein binding (% unbound) 78.210 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 15.276 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 1
pppb Pig plasma protein binding (% unbound) 80.870 % High 1
rh-clint Rat hepatocyte intrinsic clearance 9.419 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 93.580 % High 1
rppb Rat plasma protein binding (% unbound) 63.740 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 1000 uM High 1

Approvals:

DateAgencyCompanyOrphan
July 8, 1999 EMA
Dec. 17, 1998 FDA VIIV HLTHCARE

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
Food allergy 709.46 46.64 242 17100 25236 90585869
Schizophrenia 658.17 46.64 201 17141 14713 90596392
Immunodeficiency 601.84 46.64 247 17095 42987 90568118
Temperature regulation disorder 582.13 46.64 182 17160 14397 90596708
Foetal death 577.45 46.64 197 17145 20526 90590579
Exposure during pregnancy 568.80 46.64 423 16919 237987 90373118
Hypomania 528.61 46.64 151 17191 8746 90602359
Rash erythematous 486.92 46.64 241 17101 64863 90546242
Jaundice cholestatic 467.15 46.64 141 17201 9902 90601203
Cholelithiasis 415.31 46.64 202 17140 52304 90558801
Intentional product misuse 411.92 46.64 240 17102 89364 90521741
Prescribed overdose 408.33 46.64 246 17096 97379 90513726
Hepatic enzyme increased 380.34 46.64 403 16939 360333 90250772
Upper respiratory tract infection 342.25 46.64 244 17098 128074 90483031
Hyperhidrosis 340.32 46.64 249 17093 136056 90475049
Viral mutation identified 325.74 46.64 76 17266 1949 90609156
Psychotic disorder 317.56 46.64 143 17199 31087 90580018
Coeliac disease 303.52 46.64 155 17187 44455 90566650
Asthma-chronic obstructive pulmonary disease overlap syndrome 299.26 46.64 85 17257 4814 90606291
Total lung capacity increased 297.19 46.64 85 17257 4936 90606169
Hepatotoxicity 296.65 46.64 154 17188 45688 90565417
Overdose 289.10 46.64 240 17102 157469 90453636
Blood bilirubin increased 286.94 46.64 148 17194 43322 90567783
Thrombocytopenia 277.88 46.64 265 17077 208460 90402645
Fluid retention 271.07 46.64 183 17159 87908 90523197
Virologic failure 262.41 46.64 65 17277 2159 90608946
Sarcoidosis 234.17 46.64 85 17257 10588 90600517
Nasal polyps 232.58 46.64 85 17257 10795 90600310
Asthma 202.15 46.64 240 17102 241920 90369185
Rhinitis allergic 196.85 46.64 85 17257 16700 90594405
Pathogen resistance 194.47 46.64 69 17273 8046 90603059
Cardiac murmur 193.47 46.64 86 17256 18108 90592997
Psoriasis 191.50 46.64 185 17157 147569 90463536
Bronchiectasis 176.64 46.64 86 17256 22244 90588861
Product use issue 172.28 46.64 260 17082 329659 90281446
Bursitis 150.48 46.64 154 17188 131500 90479605
Drug resistance 148.83 46.64 85 17257 30364 90580741
Hypersensitivity 143.71 46.64 287 17055 454390 90156715
Immune reconstitution inflammatory syndrome 139.54 46.64 52 17290 6967 90604138
Hypertension 138.87 46.64 284 17058 457248 90153857
Lung neoplasm malignant 138.42 46.64 75 17267 24198 90586907
Rheumatoid arthritis 133.10 46.64 244 17098 362370 90248735
Treatment failure 121.05 46.64 212 17130 303716 90307389
Decreased immune responsiveness 118.19 46.64 49 17293 8699 90602406
Infusion related reaction 113.93 46.64 248 17094 416532 90194573
Pyrexia 108.54 46.64 324 17018 660161 89950944
Arthralgia 104.80 46.64 13 17329 778509 89832596
Lipodystrophy acquired 100.30 46.64 28 17314 1486 90609619
Treatment noncompliance 97.22 46.64 80 17262 51647 90559458
Chronic obstructive pulmonary disease 94.68 46.64 92 17250 73737 90537368
Blood HIV RNA increased 91.78 46.64 23 17319 801 90610304
Erythema 87.43 46.64 157 17185 229089 90382016
CD4 lymphocytes decreased 81.80 46.64 24 17318 1523 90609582
Joint swelling 81.65 46.64 246 17096 503054 90108051
Dyspnoea 77.51 46.64 36 17306 880919 89730186
Diarrhoea 75.76 46.64 43 17299 939147 89671958
Foetal exposure during pregnancy 75.64 46.64 64 17278 42911 90568194
Abdominal discomfort 72.03 46.64 5 17337 477323 90133782
Alopecia 69.72 46.64 7 17335 495064 90116041
Constipation 66.62 46.64 158 17184 280237 90330868
Peripheral swelling 66.40 46.64 3 17339 413103 90198002
Swelling 64.36 46.64 4 17338 419054 90192051
Contraindicated product administered 64.09 46.64 169 17173 319970 90291135
Dizziness 61.99 46.64 18 17324 589266 90021839
Infection 61.49 46.64 180 17162 361914 90249191
Rash 60.46 46.64 306 17036 795794 89815311
Back pain 58.04 46.64 162 17180 317013 90294092
Confusional state 55.57 46.64 5 17337 386200 90224905
Drug intolerance 53.10 46.64 197 17145 447394 90163711
Off label use 53.09 46.64 376 16966 1101876 89509229
Pruritus 50.92 46.64 20 17322 541505 90069600
Abdominal pain upper 48.69 46.64 4 17338 332670 90278435
Malaise 48.34 46.64 26 17316 585960 90025145
Weight increased 47.29 46.64 11 17331 417916 90193189

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
Lipodystrophy acquired 687.49 16.36 170 13544 3280 42604341
Immune reconstitution inflammatory syndrome 482.60 16.36 164 13550 9979 42597642
Virologic failure 472.06 16.36 130 13584 3864 42603757
Mitochondrial toxicity 442.01 16.36 113 13601 2502 42605119
Viral mutation identified 364.12 16.36 102 13612 3229 42604392
Progressive external ophthalmoplegia 355.23 16.36 84 13630 1327 42606294
Eyelid ptosis 345.61 16.36 115 13599 6546 42601075
Pathogen resistance 250.80 16.36 105 13609 11345 42596276
Diplopia 190.64 16.36 104 13610 20212 42587409
Drug resistance 116.63 16.36 93 13621 34155 42573466
Lipoatrophy 114.64 16.36 27 13687 418 42607203
Ophthalmoplegia 114.12 16.36 38 13676 2162 42605459
Drug interaction 113.83 16.36 259 13455 266740 42340881
Polydactyly 113.30 16.36 33 13681 1201 42606420
Blood HIV RNA increased 100.88 16.36 32 13682 1559 42606062
CSF HIV escape syndrome 99.81 16.36 21 13693 187 42607434
Dyslipidaemia 98.93 16.36 52 13662 9366 42598255
HIV-associated neurocognitive disorder 89.04 16.36 21 13693 327 42607294
Multiple-drug resistance 78.53 16.36 41 13673 7281 42600340
Off label use 77.44 16.36 56 13658 638279 41969342
Fanconi syndrome acquired 77.37 16.36 28 13686 2042 42605579
Foetal exposure during pregnancy 76.59 16.36 85 13629 47226 42560395
Renal impairment 73.35 16.36 129 13585 110099 42497522
Osteonecrosis 64.74 16.36 48 13666 15817 42591804
CD4 lymphocytes decreased 64.46 16.36 24 13690 1897 42605724
Hypertriglyceridaemia 63.62 16.36 40 13674 10086 42597535
Atrioventricular septal defect 62.48 16.36 15 13699 253 42607368
Viral load increased 57.37 16.36 25 13689 2972 42604649
Dandy-Walker syndrome 56.84 16.36 14 13700 264 42607357
Hyperlactacidaemia 56.32 16.36 28 13686 4488 42603133
Blood lactic acid increased 56.21 16.36 34 13680 8005 42599616
Oral candidiasis 53.06 16.36 41 13673 14364 42593257
Treatment noncompliance 53.05 16.36 63 13651 37609 42570012
Gene mutation 51.64 16.36 20 13694 1761 42605860
Trisomy 21 50.94 16.36 15 13699 567 42607054
Mitochondrial myopathy 50.51 16.36 12 13702 193 42607428
Neurodevelopmental disorder 49.91 16.36 14 13700 444 42607177
Macrocephaly 49.06 16.36 14 13700 473 42607148
Acquired immunodeficiency syndrome 48.47 16.36 14 13700 494 42607127
Oesophageal candidiasis 47.76 16.36 27 13687 5608 42602013
Herpes virus infection 46.36 16.36 23 13691 3669 42603952
Cachexia 45.92 16.36 30 13684 8074 42599547
Nervous system disorder 44.70 16.36 40 13674 17155 42590466
Congenital central nervous system anomaly 43.95 16.36 14 13700 691 42606930
White matter lesion 42.99 16.36 15 13699 983 42606638
Progressive multifocal leukoencephalopathy 42.85 16.36 33 13681 11503 42596118
Mitochondrial cytopathy 42.68 16.36 10 13704 151 42607470
Life expectancy shortened 41.38 16.36 8 13706 44 42607577
Attention deficit hyperactivity disorder 40.93 16.36 20 13694 3088 42604533
Hyperlipidaemia 40.69 16.36 42 13672 21474 42586147
Transplant rejection 40.14 16.36 34 13680 13554 42594067
Kaposi's sarcoma 38.33 16.36 13 13701 782 42606839
Blood triglycerides increased 37.46 16.36 35 13679 15861 42591760
HIV infection 37.18 16.36 15 13699 1470 42606151
Genotype drug resistance test positive 36.62 16.36 14 13700 1190 42606431
Nephropathy toxic 35.75 16.36 35 13679 16803 42590818
Pre-eclampsia 35.69 16.36 7 13707 42 42607579
HIV associated nephropathy 34.87 16.36 10 13704 344 42607277
Calculus urinary 34.75 16.36 15 13699 1742 42605879
Facial wasting 34.13 16.36 8 13706 121 42607500
Hepatitis C 33.36 16.36 27 13687 10106 42597515
Portal hypertension 32.83 16.36 20 13694 4767 42602854
Bone metabolism disorder 32.79 16.36 9 13705 263 42607358
Fall 31.78 16.36 18 13696 234502 42373119
Fanconi syndrome 31.22 16.36 14 13700 1780 42605841
Speech disorder developmental 30.98 16.36 15 13699 2270 42605351
Retinal toxicity 30.94 16.36 10 13704 517 42607104
Bacterial pyelonephritis 30.88 16.36 9 13705 328 42607293
Renal tubular disorder 29.85 16.36 19 13695 4890 42602731
Trimethylaminuria 29.72 16.36 5 13709 10 42607611
Drug ineffective 29.69 16.36 104 13610 630093 41977528
Retroperitoneal disorder 29.55 16.36 6 13708 44 42607577
Myocardial infarction 29.19 16.36 97 13617 123912 42483709
Pyrexia 28.91 16.36 221 13493 393821 42213800
Enterovirus infection 28.76 16.36 12 13702 1281 42606340
Taeniasis 28.56 16.36 6 13708 53 42607568
Gamma-glutamyltransferase increased 28.30 16.36 43 13671 32454 42575167
HIV viraemia 28.16 16.36 6 13708 57 42607564
Choroiditis 28.05 16.36 12 13702 1363 42606258
Human immunodeficiency virus transmission 27.89 16.36 6 13708 60 42607561
Varices oesophageal 26.80 16.36 17 13697 4348 42603273
COVID-19 26.79 16.36 3 13711 115945 42491676
Crystal urine 26.59 16.36 6 13708 76 42607545
Lactic acidosis 26.29 16.36 50 13664 45211 42562410
Primary syphilis 26.10 16.36 5 13709 26 42607595
Dyspnoea 25.87 16.36 66 13648 442555 42165066
Renal aneurysm 25.55 16.36 7 13707 203 42607418
Proteinuria 25.29 16.36 34 13680 22949 42584672
Coronary artery disease 24.85 16.36 54 13660 53666 42553955
Glycosuria 24.83 16.36 11 13703 1359 42606262
Mycobacterium avium complex infection 24.30 16.36 14 13700 3013 42604608
Brain oedema 24.13 16.36 28 13686 16299 42591322
Loss of anatomical alignment after fracture reduction 23.78 16.36 4 13710 8 42607613
Enterococcal infection 23.66 16.36 24 13690 12015 42595606
Heart transplant rejection 23.64 16.36 11 13703 1523 42606098
Pulmonary tuberculosis 23.24 16.36 17 13697 5484 42602137
Nephrocalcinosis 23.22 16.36 9 13705 794 42606827
Fracture malunion 22.89 16.36 4 13710 11 42607610
Glucose tolerance impaired 22.71 16.36 15 13699 4109 42603512
Musculoskeletal toxicity 22.68 16.36 6 13708 152 42607469
Coccidioidomycosis 22.60 16.36 9 13705 853 42606768
Endocardial fibroelastosis 22.39 16.36 4 13710 13 42607608
Jaundice 22.33 16.36 40 13674 34549 42573072
Pain 21.91 16.36 28 13686 244820 42362801
Hepatic function abnormal 21.79 16.36 50 13664 51517 42556104
Blood insulin increased 21.66 16.36 7 13707 362 42607259
Atrial fibrillation 21.50 16.36 9 13705 139584 42468037
Febrile neutropenia 21.45 16.36 17 13697 185686 42421935
Lymphadenopathy 20.80 16.36 38 13676 33327 42574294
Meningitis cryptococcal 20.69 16.36 13 13701 3270 42604351
Pancreatic failure 20.58 16.36 9 13705 1078 42606543
Hepatic fibrosis 20.45 16.36 15 13699 4857 42602764
Anogenital warts 20.41 16.36 8 13706 727 42606894
Post transplant distal limb syndrome 20.19 16.36 7 13707 450 42607171
Erythema elevatum diutinum 20.12 16.36 4 13710 26 42607595
Renal tubular necrosis 19.96 16.36 27 13687 18327 42589294
Coronary ostial stenosis 19.70 16.36 5 13709 107 42607514
Tuberculosis 19.60 16.36 20 13694 10079 42597542
Abdominal sepsis 19.59 16.36 9 13705 1211 42606410
Megacolon 19.50 16.36 11 13703 2274 42605347
Portal venous gas 19.45 16.36 7 13707 502 42607119
Peripheral swelling 19.26 16.36 3 13711 90267 42517354
Peripheral venous disease 19.08 16.36 12 13702 3024 42604597
Cerebral disorder 19.03 16.36 12 13702 3038 42604583
Acute myocardial infarction 18.88 16.36 51 13663 58114 42549507
Hepatitis A 18.70 16.36 7 13707 561 42607060
Renal infarct 18.65 16.36 10 13704 1873 42605748
Constipation 18.56 16.36 15 13699 162276 42445345
Blood pressure increased 18.42 16.36 5 13709 101923 42505698
Segmented hyalinising vasculitis 18.33 16.36 4 13710 43 42607578
Hepatitis B 18.21 16.36 16 13698 6695 42600926
Skin test negative 18.16 16.36 4 13710 45 42607576
Metabolic syndrome 18.16 16.36 10 13704 1973 42605648
Nephrolithiasis 18.15 16.36 38 13676 36792 42570829
Congenital pigmentation disorder 17.83 16.36 3 13711 6 42607615
Cerebral toxoplasmosis 17.63 16.36 10 13704 2088 42605533
Ophthalmic herpes simplex 17.45 16.36 6 13708 376 42607245
Tubulointerstitial nephritis 17.27 16.36 34 13680 31514 42576107
Induration 17.23 16.36 8 13706 1102 42606519
Hepatomegaly 17.06 16.36 20 13694 11765 42595856
Graft complication 17.04 16.36 7 13707 719 42606902
Hepatitis D 17.04 16.36 4 13710 61 42607560
Mesenteric artery thrombosis 16.96 16.36 7 13707 727 42606894
Blood alkaline phosphatase increased 16.95 16.36 35 13679 33562 42574059
Acute hepatic failure 16.89 16.36 24 13690 17049 42590572
Product dose omission issue 16.75 16.36 15 13699 154350 42453271
Cytomegalovirus chorioretinitis 16.70 16.36 13 13701 4598 42603023
Conjunctival pallor 16.47 16.36 4 13710 71 42607550
Graft infection 16.44 16.36 6 13708 448 42607173
Pneumonia 16.42 16.36 75 13639 422074 42185547

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
Lipodystrophy acquired 768.65 21.12 184 25431 4340 110559344
Viral mutation identified 690.49 21.12 168 25447 4251 110559433
Virologic failure 686.48 21.12 171 25444 4781 110558903
Immune reconstitution inflammatory syndrome 595.40 21.12 199 25416 16027 110547657
Schizophrenia 571.02 21.12 208 25407 21618 110542066
Hypomania 487.78 21.12 153 25462 10057 110553627
Foetal death 484.18 21.12 170 25445 15875 110547809
Mitochondrial toxicity 479.65 21.12 118 25497 3127 110560557
Temperature regulation disorder 461.39 21.12 155 25460 12671 110551013
Pathogen resistance 427.43 21.12 159 25456 17513 110546171
Food allergy 401.62 21.12 157 25458 19791 110543893
Jaundice cholestatic 396.15 21.12 143 25472 14465 110549219
Cholelithiasis 393.65 21.12 221 25394 63201 110500483
Progressive external ophthalmoplegia 387.61 21.12 85 25530 1335 110562349
Immunodeficiency 353.94 21.12 175 25440 38663 110525021
Eyelid ptosis 304.38 21.12 115 25500 13212 110550472
Total lung capacity increased 288.16 21.12 87 25528 5025 110558659
Asthma-chronic obstructive pulmonary disease overlap syndrome 269.66 21.12 87 25528 6257 110557427
Coeliac disease 269.26 21.12 151 25464 43036 110520648
Hepatic enzyme increased 265.02 21.12 348 25267 320544 110243140
Psychotic disorder 261.57 21.12 157 25458 50780 110512904
Hepatotoxicity 251.71 21.12 166 25449 63234 110500450
Blood bilirubin increased 242.77 21.12 174 25441 75798 110487886
Drug resistance 241.93 21.12 155 25460 56219 110507465
Exposure during pregnancy 222.53 21.12 232 25383 167192 110396492
Sarcoidosis 211.55 21.12 87 25528 12492 110551192
Nasal polyps 207.50 21.12 87 25528 13113 110550571
Prescribed overdose 199.44 21.12 164 25451 87417 110476267
Rash erythematous 196.38 21.12 158 25457 81674 110482010
Blood HIV RNA increased 189.37 21.12 52 25563 2136 110561548
Rhinitis allergic 185.04 21.12 88 25527 17834 110545850
Fluid retention 176.84 21.12 158 25457 94149 110469535
Cardiac murmur 164.12 21.12 90 25525 24538 110539146
Diplopia 150.18 21.12 103 25512 41791 110521893
Intentional product misuse 141.48 21.12 164 25451 132740 110430944
Bronchiectasis 133.84 21.12 91 25524 36402 110527282
Upper respiratory tract infection 129.76 21.12 156 25459 131172 110432512
CSF HIV escape syndrome 129.39 21.12 27 25588 330 110563354
Psoriasis 128.14 21.12 160 25455 139833 110423851
Treatment failure 125.65 21.12 228 25387 277006 110286678
Dyslipidaemia 125.10 21.12 65 25550 15900 110547784
Bursitis 122.94 21.12 151 25464 129767 110433917
Drug interaction 120.77 21.12 319 25296 499864 110063820
Hyperhidrosis 111.40 21.12 174 25441 187124 110376560
Treatment noncompliance 111.21 21.12 109 25506 72881 110490803
Lipoatrophy 108.75 21.12 26 25589 608 110563076
Decreased immune responsiveness 107.88 21.12 50 25565 9556 110554128
Lung neoplasm malignant 106.86 21.12 77 25538 33765 110529919
Ophthalmoplegia 104.69 21.12 37 25578 3513 110560171
CD4 lymphocytes decreased 103.20 21.12 35 25580 2939 110560745
Fanconi syndrome acquired 98.62 21.12 34 25581 3000 110560684
HIV-associated neurocognitive disorder 98.01 21.12 22 25593 386 110563298
Thrombocytopenia 89.73 21.12 228 25387 348657 110215027
Fall 85.18 21.12 18 25597 603464 109960220
Overdose 83.54 21.12 174 25441 233620 110330064
Arthralgia 77.70 21.12 42 25573 779590 109784094
Peripheral swelling 77.13 21.12 4 25611 404030 110159654
Dyspnoea 77.01 21.12 86 25529 1106786 109456898
Pyrexia 71.57 21.12 402 25213 897863 109665821
Multiple-drug resistance 65.84 21.12 40 25575 13195 110550489
Abdominal discomfort 63.89 21.12 8 25607 393850 110169834
Hypersensitivity 61.96 21.12 220 25395 403778 110159906
Nasopharyngitis 61.62 21.12 9 25606 394352 110169332
Swelling 59.78 21.12 6 25609 351035 110212649
Nephropathy toxic 59.47 21.12 50 25565 27428 110536256
Viral load increased 58.87 21.12 24 25591 3366 110560318
Renal impairment 57.88 21.12 132 25483 188313 110375371
Product use issue 56.87 21.12 180 25435 311515 110252169
Mitochondrial cytopathy 56.52 21.12 14 25601 381 110563303
Sinusitis 56.41 21.12 3 25612 296685 110266999
Hypertriglyceridaemia 56.18 21.12 39 25576 16115 110547569
Alopecia 55.44 21.12 9 25606 364744 110198940
Asthma 54.61 21.12 154 25461 250137 110313547
Blood lactic acid increased 54.57 21.12 38 25577 15783 110547901
Chronic obstructive pulmonary disease 53.50 21.12 93 25522 109065 110454619
Hypertension 52.89 21.12 246 25369 509838 110053846
Erythema 50.16 21.12 165 25450 291282 110272402
Cachexia 49.03 21.12 33 25582 12972 110550712
Contraindicated product administered 48.63 21.12 147 25468 248120 110315564
Hepatitis C 47.63 21.12 32 25583 12541 110551143
Abortion spontaneous 46.34 21.12 48 25567 34234 110529450
Hyperlactacidaemia 46.32 21.12 27 25588 8259 110555425
COVID-19 45.00 21.12 3 25612 245057 110318627
Mitochondrial myopathy 44.95 21.12 12 25603 442 110563242
Dizziness 44.46 21.12 58 25557 698135 109865549
Systemic lupus erythematosus 44.21 21.12 4 25611 254334 110309350
Retinal toxicity 44.05 21.12 16 25599 1643 110562041
HIV viraemia 42.76 21.12 9 25606 115 110563569
HIV associated nephropathy 42.73 21.12 11 25604 351 110563333
Stomatitis 42.59 21.12 6 25609 270236 110293448
Completed suicide 41.63 21.12 4 25611 242377 110321307
Confusional state 41.40 21.12 29 25586 468651 110095033
Product dose omission issue 40.69 21.12 12 25603 321770 110241914
Mycobacterium avium complex infection 40.59 21.12 22 25593 5855 110557829
Mobility decreased 40.56 21.12 4 25611 237418 110326266
Musculoskeletal stiffness 40.14 21.12 8 25607 279814 110283870
Gastroschisis 39.95 21.12 7 25608 30 110563654
Rheumatoid arthritis 39.91 21.12 156 25459 299457 110264227
Drug hypersensitivity 38.53 21.12 207 25408 453883 110109801
Discomfort 38.35 21.12 3 25612 214704 110348980
Vomiting 38.04 21.12 349 25266 910326 109653358
Therapeutic product effect incomplete 37.64 21.12 4 25611 223801 110339883
Calculus urinary 37.25 21.12 17 25598 3135 110560549
Proteinuria 36.99 21.12 46 25569 39972 110523712
Pericarditis 36.63 21.12 4 25611 219110 110344574
Transplant rejection 36.12 21.12 36 25579 24531 110539153
Blood pressure increased 35.80 21.12 8 25607 258365 110305319
Brain oedema 35.80 21.12 40 25575 31058 110532626
Weight increased 35.71 21.12 27 25588 419617 110144067
Immunosuppressant drug level increased 35.46 21.12 26 25589 11698 110551986
Herpes virus infection 35.18 21.12 23 25592 8615 110555069
Renal tubular necrosis 34.74 21.12 39 25576 30436 110533248
Impaired healing 34.44 21.12 3 25612 196714 110366970
Foetal growth abnormality 34.38 21.12 6 25609 25 110563659
Atrial fibrillation 34.14 21.12 6 25609 229636 110334048
Acquired immunodeficiency syndrome 33.27 21.12 9 25606 349 110563335
Osteonecrosis 33.15 21.12 40 25575 33701 110529983
Foetal exposure during pregnancy 33.07 21.12 21 25594 7484 110556200
Renal tubular dysfunction 32.96 21.12 11 25604 879 110562805
Retching 32.91 21.12 33 25582 22649 110541035
Back pain 32.74 21.12 171 25444 370825 110192859
Dry mouth 32.55 21.12 4 25611 199944 110363740
Lung neoplasm 31.66 21.12 21 25594 8055 110555629
Genotype drug resistance test positive 31.61 21.12 12 25603 1394 110562290
Retroperitoneal disorder 31.51 21.12 6 25609 44 110563640
Central nervous system lesion 31.00 21.12 27 25588 15526 110548158
Constipation 30.94 21.12 164 25451 357622 110206062
Lactic acidosis 30.70 21.12 67 25548 92744 110470940
Muscle spasms 30.67 21.12 13 25602 278144 110285540
Pruritus 30.56 21.12 55 25560 581505 109982179
Taeniasis 30.52 21.12 6 25609 53 110563631
Progressive multifocal leukoencephalopathy 30.28 21.12 33 25582 24923 110538761
Febrile neutropenia 30.14 21.12 18 25597 316749 110246935
Choroiditis 30.00 21.12 12 25603 1603 110562081
White matter lesion 29.88 21.12 14 25601 2740 110560944
Stillbirth 29.55 21.12 16 25599 4248 110559436
Hyperbilirubinaemia 29.54 21.12 36 25579 30635 110533049
Pulmonary tuberculosis 29.31 21.12 21 25594 9118 110554566
HIV infection 28.86 21.12 11 25604 1292 110562392
Bone metabolism disorder 28.83 21.12 9 25606 581 110563103
HIV wasting syndrome 28.78 21.12 6 25609 73 110563611
Congenital intestinal malformation 28.62 21.12 5 25610 21 110563663
Facial wasting 28.41 21.12 6 25609 78 110563606
Anxiety 28.34 21.12 23 25592 345055 110218629
Hyperlipidaemia 28.12 21.12 38 25577 35810 110527874
Drug reaction with eosinophilia and systemic symptoms 28.00 21.12 60 25555 82035 110481649
Blood triglycerides increased 27.93 21.12 31 25584 23895 110539789
Blister 27.80 21.12 9 25606 227367 110336317
Primary syphilis 27.74 21.12 5 25610 26 110563658
Glycosuria 27.40 21.12 13 25602 2617 110561067
Kaposi's sarcoma 27.29 21.12 9 25606 693 110562991
Enterovirus infection 26.76 21.12 13 25602 2757 110560927
Urticaria 26.50 21.12 21 25594 318836 110244848
Genetic polymorphism 26.24 21.12 4 25611 5 110563679
Astrocytoma malignant 26.22 21.12 5 25610 37 110563647
Renal tubular disorder 25.98 21.12 18 25597 7411 110556273
Drug intolerance 25.91 21.12 172 25443 406340 110157344
Bacterial pyelonephritis 25.86 21.12 9 25606 816 110562868
Gastrooesophageal reflux disease 25.83 21.12 96 25519 179880 110383804
Arthritis 25.75 21.12 4 25611 167582 110396102
Lymphadenopathy 25.73 21.12 50 25565 63785 110499899
Injection site pain 25.69 21.12 5 25610 177917 110385767
Foetal growth restriction 25.57 21.12 13 25602 3037 110560647
Rash 25.36 21.12 296 25319 820668 109743016
Nausea 25.36 21.12 414 25201 1235276 109328408
Infusion related reaction 25.34 21.12 163 25452 380999 110182685
Renal aneurysm 25.31 21.12 7 25608 295 110563389
Meningitis cryptococcal 25.26 21.12 15 25600 4747 110558937
Loss of anatomical alignment after fracture reduction 25.09 21.12 4 25611 8 110563676
Inappropriate schedule of product administration 25.00 21.12 8 25607 203629 110360055
Osteoarthritis 24.61 21.12 6 25609 182617 110381067
Migraine 24.42 21.12 5 25610 171647 110392037
Ocular icterus 24.36 21.12 16 25599 6037 110557647
Death 24.23 21.12 82 25533 698787 109864897
Spina bifida 23.83 21.12 6 25609 175 110563509
Fanconi syndrome 23.82 21.12 13 25602 3506 110560178
Memory impairment 23.72 21.12 8 25607 196936 110366748
Portal hypertension 23.55 21.12 18 25597 8619 110555065
Pubertal failure 23.25 21.12 4 25611 15 110563669
Coronary artery disease 22.86 21.12 51 25564 71639 110492045
Erythema elevatum diutinum 22.85 21.12 4 25611 17 110563667
Nervous system disorder 22.44 21.12 32 25583 31689 110531995
Meningitis tuberculous 22.03 21.12 9 25606 1269 110562415
Syncope 21.48 21.12 10 25605 202526 110361158
Bronchitis 21.47 21.12 5 25610 157027 110406657
Ill-defined disorder 21.43 21.12 5 25610 156848 110406836
Enterococcal infection 21.42 21.12 25 25590 20341 110543343
Portal venous gas 21.40 21.12 7 25608 525 110563159
Hypotension 21.35 21.12 57 25558 523792 110039892
Abdominal pain upper 21.17 21.12 30 25585 349081 110214603
Social avoidant behaviour 21.14 21.12 14 25601 5355 110558329

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AF06 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Nucleoside and nucleotide reverse transcriptase inhibitors
ATC J05AR02 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR04 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR13 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
FDA MoA N0000009947 Nucleoside Reverse Transcriptase Inhibitors
FDA EPC N0000175462 Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor
CHEBI has role CHEBI:50748 antipsoriatic
CHEBI has role CHEBI:64946 anti-HIV agent
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018894 Reverse Transcriptase Inhibitors
MeSH PA D019380 Anti-HIV Agents
MeSH PA D019384 Nucleic Acid Synthesis Inhibitors
FDA MoA N0000193954 Cytochrome P450 1A1 Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:33231 antitubercular agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:36044 antiviral drug
CHEBI has role CHEBI:53756 HIV-1 reverse transcriptase inhibitor
CHEBI has role CHEBI:88188 drug allergen

Related Drugs by ATC class:

J05AF Nucleoside and nucleotide reverse transcriptase inhibitors 12 drugs
adefovir dipivoxilclevudinedidanosineemtricitabineentecavirlamivudinestavudinetelbivudinetenofovir alafenamidetenofovir disoproxilzalcitabinezidovudine
J05AR Antivirals for treatment of HIV infections, combinations 19 drugs
atazanavirbictegravircobicistatdarunavirdolutegravirdoravirineefavirenzelvitegraviremtricitabinelamivudinelopinavirnevirapine 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
Toxic amblyopia contraindication 965003
Myositis contraindication 26889001 DOID:633
Hepatic failure contraindication 59927004
Pancreatitis contraindication 75694006 DOID:4989
Large liver contraindication 80515008
Kidney disease contraindication 90708001 DOID:557
Lactic acidosis contraindication 91273001 DOID:3650
Disorder of muscle contraindication 129565002 DOID:423
Steatosis of liver contraindication 197321007
Acute pancreatitis contraindication 197456007 DOID:2913
Chronic pancreatitis contraindication 235494005
Disease of liver contraindication 235856003 DOID:409
Anemia contraindication 271737000 DOID:2355
Hypertriglyceridemia contraindication 302870006
Neutropenic disorder contraindication 303011007 DOID:1227
Bone marrow depression contraindication 307762000
Breastfeeding (mother) contraindication 413712001
Obesity contraindication 414916001 DOID:9970
HLA-B 5701 Positive Status contraindication
Drug Resistance to Anti-retroviral Therapy contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.09 acidic
pKa2 5.64 Basic
pKa3 0.88 Basic
pKa4 0.28 Basic

Orange Book patent data (new drug applications)

None

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

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Reverse transcriptase/RNaseH Enzyme INHIBITOR EC50 5.28 CHEMBL CHEMBL
Gag-Pol polyprotein Polyprotein EC50 5.28 WOMBAT-PK
Reverse transcriptase Enzyme IC50 6.89 CHEMBL

External reference:

IDSource
4029879 VUID
N0000180961 NUI
D00891 KEGG_DRUG
188062-50-2 SECONDARY_CAS_RN
190521 RXNORM
C0663655 UMLSCUI
CHEBI:421707 CHEBI
1KX PDB_CHEM_ID
CHEMBL1380 ChEMBL_ID
CHEMBL2106686 ChEMBL_ID
CHEMBL4303288 ChEMBL_ID
DB01048 DRUGBANK_ID
D000099227 MESH_DESCRIPTOR_UI
441300 PUBCHEM_CID
11152 IUPHAR_LIGAND_ID
7544 INN_ID
168146-84-7 SECONDARY_CAS_RN
WR2TIP26VS UNII
14010 MMSL
191490 MMSL
30504 MMSL
66957 MMSL
7865 MMSL
d04376 MMSL
4021139 VANDF
4024130 VANDF
4029879 VANDF
007687 NDDF
007688 NDDF
116084008 SNOMEDCT_US
387005008 SNOMEDCT_US
412074007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Abacavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0378-4105 TABLET, FILM COATED 300 mg ORAL ANDA 28 sections
Abacavir HUMAN PRESCRIPTION DRUG LABEL 1 0904-6874 TABLET, FILM COATED 300 mg ORAL ANDA 27 sections
Abacavir HUMAN PRESCRIPTION DRUG LABEL 1 31722-557 TABLET 300 mg ORAL ANDA 26 sections
Abacavir Human Prescription Drug Label 1 31722-562 SOLUTION 20 mg ORAL ANDA 28 sections
ABACAVIR and LAMIVUDINE HUMAN PRESCRIPTION DRUG LABEL 2 31722-838 TABLET, FILM COATED 600 mg ORAL ANDA 27 sections
Abacavir and Lamivudine Human Prescription Drug Label 2 33342-440 TABLET, FILM COATED 600 mg ORAL ANDA 27 sections
Abacavir and Lamivudine Human Prescription Drug Label 2 42385-962 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
Abacavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 48433-001 TABLET, FILM COATED 300 mg ORAL ANDA 28 sections
ZIAGEN HUMAN PRESCRIPTION DRUG LABEL 1 49702-222 SOLUTION 20 mg ORAL NDA 26 sections
Triumeq HUMAN PRESCRIPTION DRUG LABEL 3 49702-231 TABLET, FILM COATED 600 mg ORAL NDA 27 sections
Triumeq HUMAN PRESCRIPTION DRUG LABEL 3 49702-231 TABLET, FILM COATED 600 mg ORAL NDA 27 sections
Abacavir HUMAN PRESCRIPTION DRUG LABEL 1 50268-049 TABLET 300 mg ORAL ANDA 27 sections
Abacavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 51079-204 TABLET, FILM COATED 300 mg ORAL ANDA 28 sections
Abacavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 53808-0627 TABLET, FILM COATED 300 mg ORAL ANDA 30 sections
EPZICOM HUMAN PRESCRIPTION DRUG LABEL 2 53808-0767 TABLET, FILM COATED 600 mg ORAL NDA 26 sections
ZIAGEN HUMAN PRESCRIPTION DRUG LABEL 1 53808-0811 TABLET, FILM COATED 300 mg ORAL NDA 29 sections
TRIZIVIR HUMAN PRESCRIPTION DRUG LABEL 3 53808-0990 TABLET, FILM COATED 300 mg ORAL NDA 28 sections
EPZICOM HUMAN PRESCRIPTION DRUG LABEL 2 54868-5600 TABLET, FILM COATED 600 mg ORAL NDA 26 sections
Abacavir Human Prescription Drug Label 1 64980-405 SOLUTION 20 mg ORAL ANDA 27 sections
Abacavir Human Prescription Drug Label 1 65862-073 TABLET, FILM COATED 300 mg ORAL ANDA 27 sections
Abacavir Human Prescription Drug Label 1 65862-089 SOLUTION 20 mg ORAL ANDA 27 sections
Abacavir and Lamivudine Human Prescription Drug Label 2 65862-335 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
Abacavir HUMAN PRESCRIPTION DRUG LABEL 1 67046-1602 TABLET 300 mg ORAL ANDA 25 sections
Abacavir HUMAN PRESCRIPTION DRUG LABEL 1 68084-021 TABLET, FILM COATED 300 mg ORAL ANDA 27 sections
ABACAVIR, LAMIVUDINE AND ZIDOVUDINE HUMAN PRESCRIPTION DRUG LABEL 3 68180-286 TABLET 300 mg ORAL ANDA 28 sections
Abacavir and Lamivudine HUMAN PRESCRIPTION DRUG LABEL 2 68180-288 TABLET, FILM COATED 600 mg ORAL ANDA 26 sections
Abacavir and Lamivudine HUMAN PRESCRIPTION DRUG LABEL 2 69097-362 TABLET, FILM COATED 600 mg ORAL ANDA 26 sections
Abacavir HUMAN PRESCRIPTION DRUG LABEL 1 69097-514 TABLET, FILM COATED 300 mg ORAL ANDA 25 sections
Abacavir HUMAN PRESCRIPTION DRUG LABEL 1 72865-167 TABLET 300 mg ORAL ANDA 26 sections