abacavir ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 ยตM/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

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
Exposure during pregnancy 423.97 28.17 275 9480 155272 63323995
Hypomania 346.28 28.17 96 9659 6234 63473033
Jaundice cholestatic 332.43 28.17 96 9659 7228 63472039
Viral mutation identified 323.05 28.17 71 9684 1739 63477528
Schizophrenia 307.55 28.17 97 9658 9855 63469412
Virologic failure 261.22 28.17 60 9695 1802 63477465
Hepatotoxicity 243.05 28.17 117 9638 36924 63442343
Abortion spontaneous 227.48 28.17 121 9634 47074 63432193
Psychotic disorder 224.32 28.17 99 9656 25613 63453654
Blood bilirubin increased 207.01 28.17 105 9650 37035 63442232
Foetal death 203.97 28.17 73 9682 10907 63468360
Pathogen resistance 196.12 28.17 62 9693 6336 63472931
Immune reconstitution inflammatory syndrome 195.00 28.17 61 9694 6023 63473244
Drug resistance 189.43 28.17 85 9670 22848 63456419
Cholelithiasis 174.07 28.17 99 9656 43826 63435441
Asthma-chronic obstructive pulmonary disease overlap syndrome 144.31 28.17 38 9717 2023 63477244
Total lung capacity increased 140.02 28.17 38 9717 2272 63476995
Foetal exposure during pregnancy 137.36 28.17 76 9679 31886 63447381
Lipodystrophy acquired 127.18 28.17 32 9723 1420 63477847
Hepatic enzyme increased 114.73 28.17 148 9607 202180 63277087
Nasal polyps 104.07 28.17 38 9717 6001 63473266
Treatment noncompliance 101.17 28.17 66 9689 37259 63442008
Live birth 99.41 28.17 57 9698 25573 63453694
Premature baby 99.33 28.17 53 9702 20682 63458585
Sarcoidosis 97.97 28.17 38 9717 7084 63472183
Temperature regulation disorder 92.52 28.17 35 9720 6097 63473170
Blood HIV RNA increased 88.76 28.17 21 9734 718 63478549
Stillbirth 85.75 28.17 34 9721 6716 63472551
CD4 lymphocytes decreased 84.27 28.17 23 9732 1404 63477863
Cardiac murmur 80.58 28.17 41 9714 14511 63464756
Rhinitis allergic 79.72 28.17 38 9717 11689 63467578
Abortion induced 78.32 28.17 36 9719 10206 63469061
Food allergy 77.68 28.17 37 9718 11364 63467903
Bronchiectasis 71.00 28.17 39 9716 16103 63463164
Pregnancy 66.89 28.17 51 9704 36785 63442482
Coeliac disease 64.93 28.17 34 9721 12763 63466504
Foetal growth restriction 52.94 28.17 25 9730 7528 63471739
Immunodeficiency 52.87 28.17 35 9720 20219 63459048
Fall 48.45 28.17 3 9752 392331 63086936
Lung neoplasm malignant 46.63 28.17 32 9723 19601 63459666
Trisomy 21 46.27 28.17 11 9744 384 63478883
Maternal exposure during pregnancy 45.79 28.17 103 9652 219959 63259308
Foetal growth abnormality 45.50 28.17 8 9747 57 63479210
Drug reaction with eosinophilia and systemic symptoms 44.85 28.17 39 9716 33797 63445470
Drug ineffective 44.03 28.17 58 9697 1044707 62434560
Vomiting 43.24 28.17 185 9570 559432 62919835
Arthralgia 42.93 28.17 17 9738 569693 62909574
Fanconi syndrome acquired 40.04 28.17 12 9743 1024 63478243
Infertility 38.83 28.17 11 9744 770 63478497
Astrocytoma malignant 38.37 28.17 6 9749 18 63479249
Renal tubular acidosis 38.13 28.17 13 9742 1679 63477588
Ovarian failure 37.26 28.17 12 9743 1298 63477969
Chronic obstructive pulmonary disease 37.20 28.17 47 9708 62639 63416628
Caesarean section 36.34 28.17 26 9729 17006 63462261
Placental insufficiency 36.14 28.17 12 9743 1429 63477838
Premature labour 36.04 28.17 23 9732 12481 63466786
Hyperbilirubinaemia 35.60 28.17 22 9733 11292 63467975
Gastroschisis 35.45 28.17 9 9746 414 63478853
Isoimmune haemolytic disease 34.88 28.17 6 9749 37 63479230
Nephropathy toxic 33.87 28.17 20 9735 9459 63469808
Rash erythematous 33.75 28.17 37 9718 42473 63436794
Antiviral drug level below therapeutic 32.98 28.17 6 9749 53 63479214
Prescribed overdose 32.97 28.17 33 9722 34120 63445147
Drug interaction 32.72 28.17 93 9662 229038 63250229
Viral load increased 32.70 28.17 11 9744 1363 63477904
Bursitis 32.51 28.17 34 9721 37007 63442260
Pain in extremity 32.20 28.17 6 9749 331480 63147787
Pre-eclampsia 31.93 28.17 19 9736 9114 63470153
Immunosuppressant drug level increased 31.66 28.17 14 9741 3624 63475643
Proteinuria 31.47 28.17 25 9730 19120 63460147
Peripheral swelling 30.10 28.17 3 9752 265939 63213328
Foetal anaemia 29.70 28.17 6 9749 96 63479171
Mitochondrial toxicity 29.55 28.17 8 9747 473 63478794
Congenital intestinal malformation 29.04 28.17 5 9750 31 63479236
Abdominal discomfort 28.73 28.17 7 9748 320878 63158389
Ultrasound scan abnormal 28.54 28.17 7 9748 279 63478988

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 592.45 15.27 161 15686 3183 34937901
Immune reconstitution inflammatory syndrome 526.82 15.27 184 15663 8575 34932509
Mitochondrial toxicity 418.22 15.27 117 15730 2582 34938502
Virologic failure 414.87 15.27 123 15724 3357 34937727
Viral mutation identified 337.29 15.27 101 15746 2853 34938231
Progressive external ophthalmoplegia 320.32 15.27 83 15764 1352 34939732
Eyelid ptosis 285.72 15.27 105 15742 5661 34935423
Pathogen resistance 209.87 15.27 97 15750 9385 34931699
Diplopia 183.43 15.27 107 15740 16736 34924348
Polydactyly 115.13 15.27 36 15811 1177 34939907
Drug resistance 111.33 15.27 93 15754 25834 34915250
Lipoatrophy 106.51 15.27 28 15819 483 34940601
Blood HIV RNA increased 98.18 15.27 32 15815 1198 34939886
Drug interaction 96.99 15.27 272 15575 225674 34715410
Foetal exposure during pregnancy 94.86 15.27 101 15746 38000 34903084
CSF HIV escape syndrome 93.35 15.27 21 15826 180 34940904
Ophthalmoplegia 92.93 15.27 34 15813 1806 34939278
HIV-associated neurocognitive disorder 87.06 15.27 22 15825 322 34940762
Dyslipidaemia 77.35 15.27 46 15801 7442 34933642
Exposure during pregnancy 77.28 15.27 49 15798 8885 34932199
Off label use 72.68 15.27 51 15796 419473 34521611
Fanconi syndrome acquired 72.55 15.27 29 15818 1962 34939122
Renal impairment 68.91 15.27 140 15707 94373 34846711
Multiple-drug resistance 67.01 15.27 37 15810 5202 34935882
Trisomy 21 66.67 15.27 20 15827 567 34940517
Atrioventricular septal defect 64.37 15.27 16 15831 218 34940866
Osteonecrosis 63.04 15.27 53 15794 14837 34926247
Viral load increased 62.67 15.27 28 15819 2499 34938585
Hypertriglyceridaemia 62.46 15.27 42 15805 8406 34932678
CD4 lymphocytes decreased 62.20 15.27 25 15822 1716 34939368
Hyperlipidaemia 62.10 15.27 52 15795 14477 34926607
Kaposi's sarcoma 58.64 15.27 20 15827 863 34940221
Hyperlactacidaemia 57.93 15.27 28 15819 2988 34938096
Dandy-Walker syndrome 55.39 15.27 14 15833 205 34940879
Gene mutation 53.02 15.27 21 15826 1387 34939697
Mitochondrial cytopathy 52.18 15.27 13 15834 179 34940905
Acquired immunodeficiency syndrome 51.79 15.27 16 15831 502 34940582
Oral candidiasis 48.99 15.27 42 15805 12068 34929016
Cachexia 46.70 15.27 33 15814 7153 34933931
Mitochondrial myopathy 46.43 15.27 12 15835 193 34940891
Progressive multifocal leukoencephalopathy 46.02 15.27 37 15810 9727 34931357
Neurodevelopmental disorder 45.82 15.27 14 15833 423 34940661
Pyrexia 45.72 15.27 282 15565 332731 34608353
Oesophageal candidiasis 45.38 15.27 27 15820 4369 34936715
Treatment noncompliance 44.25 15.27 59 15788 28041 34913043
Macrocephaly 43.74 15.27 14 15833 494 34940590
HIV infection 43.63 15.27 18 15829 1321 34939763
Blood triglycerides increased 43.35 15.27 42 15805 14117 34926967
Life expectancy shortened 42.67 15.27 9 15838 55 34941029
Blood lactic acid increased 41.66 15.27 30 15817 6698 34934386
Fall 41.62 15.27 20 15827 202865 34738219
Congenital central nervous system anomaly 40.96 15.27 14 15833 608 34940476
White matter lesion 40.95 15.27 15 15832 799 34940285
Nervous system disorder 40.56 15.27 41 15806 14502 34926582
Cytomegalovirus chorioretinitis 39.56 15.27 23 15824 3566 34937518
Meningitis cryptococcal 39.30 15.27 20 15827 2384 34938700
Drug ineffective 37.66 15.27 96 15751 456655 34484429
Retinal toxicity 37.37 15.27 12 15835 428 34940656
Nephrolithiasis 36.45 15.27 56 15791 30277 34910807
Fanconi syndrome 36.18 15.27 17 15830 1703 34939381
Mycobacterium avium complex infection 35.63 15.27 19 15828 2492 34938592
Lactic acidosis 34.69 15.27 59 15788 34713 34906371
Nephropathy toxic 34.22 15.27 35 15812 12553 34928531
Hepatitis C 33.61 15.27 31 15816 9799 34931285
Genotype drug resistance test positive 32.65 15.27 14 15833 1131 34939953
Pre-eclampsia 32.24 15.27 7 15840 50 34941034
HIV associated nephropathy 32.09 15.27 10 15837 323 34940761
Portal hypertension 31.97 15.27 21 15826 4041 34937043
Jaundice 31.68 15.27 54 15793 31828 34909256
Liver disorder 31.62 15.27 55 15792 32942 34908142
Enterovirus infection 31.26 15.27 13 15834 973 34940111
Completed suicide 30.92 15.27 4 15843 98164 34842920
Bone metabolism disorder 30.56 15.27 9 15838 239 34940845
Bacterial pyelonephritis 30.21 15.27 9 15838 249 34940835
Atrial fibrillation 30.18 15.27 9 15838 122384 34818700
Cerebral toxoplasmosis 30.13 15.27 15 15832 1706 34939378
Calculus urinary 29.89 15.27 14 15833 1393 34939691
Facial wasting 29.85 15.27 8 15839 149 34940935
Human immunodeficiency virus transmission 29.80 15.27 6 15841 28 34941056
Renal tubular disorder 29.42 15.27 21 15826 4622 34936462
Speech disorder developmental 29.41 15.27 16 15831 2184 34938900
Trimethylaminuria 28.01 15.27 5 15842 10 34941074
Proteinuria 27.60 15.27 38 15809 18604 34922480
Premature baby 27.55 15.27 39 15808 19594 34921490
Neonatal asphyxia 27.38 15.27 9 15838 346 34940738
HIV viraemia 27.04 15.27 6 15841 48 34941036
Transplant rejection 26.82 15.27 28 15819 10283 34930801
Taeniasis 26.51 15.27 6 15841 53 34941031
Anogenital warts 26.37 15.27 10 15837 587 34940497
Dyspnoea 26.02 15.27 86 15761 376696 34564388
Primary syphilis 25.88 15.27 5 15842 18 34941066
Pain 25.78 15.27 33 15814 204642 34736442
Choroiditis 25.53 15.27 12 15835 1203 34939881
Small for dates baby 25.43 15.27 18 15829 3909 34937175
Hepatic fibrosis 25.05 15.27 19 15828 4588 34936496
Drug abuse 24.96 15.27 7 15840 99089 34841995
Crystal urine 24.54 15.27 6 15841 76 34941008
Gamma-glutamyltransferase increased 24.53 15.27 46 15801 29185 34911899
Pulmonary tuberculosis 24.52 15.27 19 15828 4735 34936349
Constipation 24.47 15.27 16 15831 136966 34804118
Peripheral swelling 24.39 15.27 3 15844 76538 34864546
Varices oesophageal 23.83 15.27 17 15830 3738 34937346
Myocardial infarction 23.59 15.27 113 15734 120972 34820112
Blood insulin increased 23.30 15.27 8 15839 352 34940732
Hyperbilirubinaemia 22.96 15.27 33 15814 16810 34924274
Tubulointerstitial nephritis 22.74 15.27 37 15810 20987 34920097
Loss of anatomical alignment after fracture reduction 22.41 15.27 4 15843 8 34941076
Subchondral insufficiency fracture 22.41 15.27 4 15843 8 34941076
Heart transplant rejection 22.36 15.27 11 15836 1220 34939864
Glycosuria 22.30 15.27 11 15836 1226 34939858
Attention deficit hyperactivity disorder 22.03 15.27 14 15833 2545 34938539
Tuberculosis 21.78 15.27 23 15824 8554 34932530
Brain oedema 21.72 15.27 29 15818 13792 34927292
Fracture malunion 21.52 15.27 4 15843 11 34941073
Hepatic function abnormal 21.50 15.27 56 15791 44307 34896777
Hepatomegaly 21.44 15.27 25 15822 10371 34930713
Coronary artery disease 21.42 15.27 59 15788 48246 34892838
Product dose omission issue 21.35 15.27 14 15833 119697 34821387
Musculoskeletal toxicity 21.32 15.27 6 15841 135 34940949
Lipohypertrophy 21.25 15.27 7 15840 271 34940813
Splenomegaly 21.17 15.27 30 15817 15087 34925997
Endocardial fibroelastosis 21.02 15.27 4 15843 13 34941071
Pneumonia 20.96 15.27 89 15758 362538 34578546
Post transplant distal limb syndrome 20.84 15.27 7 15840 288 34940796
Blood pressure increased 20.78 15.27 7 15840 88095 34852989
Coccidioidomycosis 20.63 15.27 9 15838 758 34940326
Lymphadenopathy 20.50 15.27 42 15805 28421 34912663
Pancreatic failure 20.29 15.27 9 15838 789 34940295
Blood bilirubin increased 20.29 15.27 50 15797 38246 34902838
Hypotension 19.43 15.27 45 15802 221604 34719480
Erythema elevatum diutinum 18.75 15.27 4 15843 26 34941058
Febrile neutropenia 18.34 15.27 21 15826 136828 34804256
Encephalitis 17.57 15.27 19 15828 7258 34933826
Malignant neoplasm progression 17.54 15.27 9 15838 88037 34853047
Intentional product use issue 17.53 15.27 3 15844 59813 34881271
Renal tubular necrosis 17.51 15.27 28 15819 15652 34925432
Hepatitis A 17.27 15.27 7 15840 491 34940593
Death 17.18 15.27 108 15739 397941 34543143
Cerebral disorder 17.03 15.27 12 15835 2589 34938495
Congenital pigmentation disorder 16.81 15.27 3 15844 6 34941078
Skin test negative 16.80 15.27 4 15843 45 34941039
Pancreatitis 16.74 15.27 47 15800 38844 34902240
Segmented hyalinising vasculitis 16.72 15.27 4 15843 46 34941038
Peripheral venous disease 16.67 15.27 12 15835 2676 34938408
Glucose tolerance impaired 16.59 15.27 13 15834 3291 34937793
Pancytopenia 16.53 15.27 86 15761 95071 34846013
Hepatitis D 16.48 15.27 4 15843 49 34941035
Blood uric acid increased 16.37 15.27 21 15826 9603 34931481
Ophthalmic herpes simplex 16.30 15.27 6 15841 324 34940760
Disease progression 16.28 15.27 15 15832 108062 34833022
Pharyngitis 16.21 15.27 19 15828 7925 34933159
Conjunctival pallor 16.20 15.27 4 15843 53 34941031
Herpes virus infection 16.07 15.27 12 15835 2830 34938254
Polyneuropathy 15.82 15.27 26 15821 14870 34926214
Blood alkaline phosphatase increased 15.77 15.27 40 15807 31135 34909949
Normal newborn 15.69 15.27 5 15842 174 34940910
Induration 15.61 15.27 8 15839 967 34940117
Amoebiasis 15.32 15.27 4 15843 67 34941017

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 713.87 16.60 176 20717 4149 79719346
Immune reconstitution inflammatory syndrome 696.18 16.60 222 20671 13619 79709876
Viral mutation identified 662.08 16.60 162 20731 3696 79719799
Virologic failure 604.00 16.60 153 20740 4038 79719457
Mitochondrial toxicity 490.09 16.60 122 20771 2992 79720503
Pathogen resistance 381.61 16.60 143 20750 14199 79709296
Progressive external ophthalmoplegia 370.32 16.60 84 20809 1361 79722134
Hypomania 278.96 16.60 96 20797 7448 79716047
Eyelid ptosis 275.25 16.60 105 20788 10939 79712556
Drug resistance 263.13 16.60 154 20739 42059 79681436
Exposure during pregnancy 249.95 16.60 209 20684 100923 79622572
Jaundice cholestatic 241.28 16.60 96 20797 11188 79712307
Schizophrenia 225.03 16.60 100 20793 15340 79708155
Abortion spontaneous 190.06 16.60 110 20783 29397 79694098
Hepatotoxicity 187.81 16.60 134 20759 51218 79672277
Blood HIV RNA increased 178.84 16.60 49 20844 1759 79721736
Blood bilirubin increased 170.02 16.60 140 20753 66092 79657403
Diplopia 169.68 16.60 107 20786 33359 79690136
Psychotic disorder 160.57 16.60 112 20781 41290 79682205
Foetal death 160.08 16.60 65 20828 7979 79715516
Cholelithiasis 145.02 16.60 116 20777 52548 79670947
Drug interaction 126.53 16.60 312 20581 414871 79308624
CSF HIV escape syndrome 121.16 16.60 26 20867 321 79723174
Total lung capacity increased 120.14 16.60 38 20855 2260 79721235
Lipoatrophy 108.41 16.60 27 20866 662 79722833
Asthma-chronic obstructive pulmonary disease overlap syndrome 107.56 16.60 38 20855 3183 79720312
HIV-associated neurocognitive disorder 104.04 16.60 23 20870 329 79723166
Hepatic enzyme increased 102.80 16.60 177 20716 182433 79541062
CD4 lymphocytes decreased 99.22 16.60 34 20859 2600 79720895
Treatment noncompliance 99.00 16.60 93 20800 52175 79671320
Dyslipidaemia 95.79 16.60 51 20842 11582 79711913
Fanconi syndrome acquired 94.61 16.60 33 20860 2661 79720834
Ophthalmoplegia 92.10 16.60 33 20860 2879 79720616
Nasal polyps 77.40 16.60 38 20855 7289 79716206
Viral load increased 76.93 16.60 29 20864 2919 79720576
Sarcoidosis 72.76 16.60 38 20855 8297 79715198
Fall 70.95 16.60 20 20873 487609 79235886
Hypertriglyceridaemia 70.28 16.60 43 20850 12697 79710798
Stillbirth 68.68 16.60 29 20864 3926 79719569
Abortion induced 66.64 16.60 34 20859 7075 79716420
Renal impairment 66.32 16.60 135 20758 157648 79565847
Nephropathy toxic 64.92 16.60 49 20844 20370 79703125
Mitochondrial cytopathy 64.17 16.60 16 20877 394 79723101
Multiple-drug resistance 62.50 16.60 35 20858 8773 79714722
Live birth 61.86 16.60 46 20847 18698 79704797
Rhinitis allergic 61.59 16.60 39 20854 12230 79711265
Temperature regulation disorder 60.76 16.60 30 20863 5823 79717672
Cardiac murmur 59.43 16.60 42 20851 15782 79707713
Pyrexia 58.83 16.60 340 20553 678369 79045126
Peripheral swelling 55.26 16.60 4 20889 269613 79453882
Hyperlipidaemia 54.39 16.60 49 20844 26044 79697451
Hyperlactacidaemia 53.14 16.60 27 20866 5568 79717927
Cachexia 52.58 16.60 34 20859 11049 79712446
Retinal toxicity 52.32 16.60 18 20875 1393 79722102
Pain 50.92 16.60 66 20827 703736 79019759
Proteinuria 48.85 16.60 51 20842 32451 79691044
Meningitis cryptococcal 48.80 16.60 22 20871 3484 79720011
Mitochondrial myopathy 48.54 16.60 12 20881 285 79723210
Food allergy 48.40 16.60 32 20861 10792 79712703
Blood lactic acid increased 48.27 16.60 34 20859 12710 79710785
Completed suicide 46.70 16.60 5 20888 245762 79477733
Bronchiectasis 46.58 16.60 42 20851 22344 79701151
Mycobacterium avium complex infection 46.04 16.60 23 20870 4577 79718918
Lactic acidosis 45.97 16.60 73 20820 70286 79653209
Immunodeficiency 45.61 16.60 41 20852 21727 79701768
Drug reaction with eosinophilia and systemic symptoms 45.24 16.60 69 20824 64175 79659320
Hyperbilirubinaemia 45.21 16.60 43 20850 24475 79699020
Drug ineffective 45.06 16.60 140 20753 1080773 78642722
Osteonecrosis 43.55 16.60 47 20846 31048 79692447
HIV viraemia 43.32 16.60 9 20884 94 79723401
Hepatitis C 43.28 16.60 31 20862 11894 79711601
Coeliac disease 42.33 16.60 30 20863 11321 79712174
HIV associated nephropathy 42.17 16.60 11 20882 326 79723169
Dyspnoea 41.63 16.60 103 20790 856922 78866573
Kaposi's sarcoma 41.54 16.60 13 20880 746 79722749
Arthralgia 40.93 16.60 54 20839 571749 79151746
Brain oedema 40.42 16.60 41 20852 25222 79698273
Sinusitis 39.76 16.60 3 20890 195498 79527997
Off label use 39.56 16.60 115 20778 907100 78816395
Gastroschisis 39.09 16.60 7 20886 30 79723465
Blood triglycerides increased 38.98 16.60 37 20856 21003 79702492
Jaundice 37.14 16.60 57 20836 53292 79670203
Abdominal discomfort 36.94 16.60 10 20883 250717 79472778
HIV infection 36.50 16.60 13 20880 1114 79722381
Product dose omission issue 36.23 16.60 10 20883 247527 79475968
Renal tubular disorder 36.05 16.60 22 20871 6464 79717031
Calculus urinary 36.04 16.60 16 20877 2444 79721051
Swelling 35.19 16.60 7 20886 216704 79506791
Glycosuria 34.55 16.60 15 20878 2173 79721322
Cytomegalovirus chorioretinitis 34.09 16.60 20 20873 5470 79718025
Nasopharyngitis 34.04 16.60 12 20881 253869 79469626
Foetal growth abnormality 33.64 16.60 6 20887 25 79723470
Renal tubular necrosis 33.59 16.60 37 20856 25002 79698493
Foetal exposure during pregnancy 33.11 16.60 20 20873 5770 79717725
Renal tubular dysfunction 33.09 16.60 11 20882 766 79722729
Nephrolithiasis 33.04 16.60 54 20839 53237 79670258
Atrial fibrillation 32.96 16.60 6 20887 197880 79525615
Enterovirus infection 32.89 16.60 14 20879 1933 79721562
White matter lesion 32.38 16.60 14 20879 2008 79721487
Pulmonary tuberculosis 32.17 16.60 22 20871 7843 79715652
Progressive multifocal leukoencephalopathy 32.17 16.60 33 20860 20567 79702928
Foetal growth restriction 31.75 16.60 14 20879 2105 79721390
Lymphadenopathy 31.73 16.60 53 20840 53194 79670301
Central nervous system lesion 31.66 16.60 27 20866 13341 79710154
Genotype drug resistance test positive 31.02 16.60 12 20881 1296 79722199
Alopecia 30.90 16.60 11 20882 231344 79492151
Fanconi syndrome 30.72 16.60 15 20878 2841 79720654
Choroiditis 30.38 16.60 12 20881 1369 79722126
Taeniasis 29.79 16.60 6 20887 53 79723442
Pancreatitis 29.16 16.60 59 20834 68516 79654979
Vomiting 29.15 16.60 284 20609 665544 79057951
Intentional product use issue 29.13 16.60 3 20890 152109 79571386
Bone metabolism disorder 28.89 16.60 9 20884 509 79722986
Acquired immunodeficiency syndrome 28.88 16.60 8 20885 299 79723196
Primary syphilis 28.83 16.60 5 20888 17 79723478
Synovitis 28.79 16.60 3 20890 150731 79572764
Tuberculosis 28.68 16.60 27 20866 15171 79708324
Transplant rejection 28.31 16.60 30 20863 19407 79704088
Blood pressure increased 28.31 16.60 10 20883 211350 79512145
HIV wasting syndrome 28.27 16.60 6 20887 70 79723425
Nervous system disorder 28.20 16.60 35 20858 26821 79696674
Bacterial pyelonephritis 28.06 16.60 9 20884 560 79722935
Congenital intestinal malformation 28 16.60 5 20888 21 79723474
Treatment failure 27.80 16.60 103 20790 170383 79553112
Renal tubular acidosis 27.39 16.60 15 20878 3599 79719896
Immunosuppressant drug level increased 27.23 16.60 21 20872 9006 79714489
Cerebral toxoplasmosis 27.21 16.60 13 20880 2349 79721146
Astrocytoma malignant 27.12 16.60 5 20888 26 79723469
Portal hypertension 27.00 16.60 19 20874 7089 79716406
Facial wasting 27.00 16.60 6 20887 88 79723407
Oesophageal candidiasis 26.84 16.60 21 20872 9197 79714298
Therapeutic product effect incomplete 26.59 16.60 3 20890 141642 79581853
Hepatic fibrosis 26.59 16.60 19 20874 7261 79716234
Lung neoplasm malignant 25.69 16.60 34 20859 27758 79695737
Infection 25.37 16.60 16 20877 241696 79481799
Pregnancy 25.06 16.60 33 20860 26818 79696677
Loss of anatomical alignment after fracture reduction 24.60 16.60 4 20889 8 79723487
Death 24.48 16.60 72 20821 566442 79157053
Gamma-glutamyltransferase increased 24.39 16.60 48 20845 54632 79668863
Spina bifida 24.17 16.60 6 20887 145 79723350
Coronary artery disease 23.97 16.60 53 20840 65421 79658074
Renal failure 23.78 16.60 110 20783 200858 79522637
Anogenital warts 23.69 16.60 9 20884 925 79722570
Encephalitis 23.69 16.60 24 20869 14736 79708759
Lower respiratory tract infection 23.61 16.60 3 20890 129217 79594278
Rash maculo-papular 23.55 16.60 48 20845 56030 79667465
Pain in extremity 23.50 16.60 37 20856 364501 79358994
New onset diabetes after transplantation 23.46 16.60 6 20887 164 79723331
Cushing's syndrome 23.14 16.60 9 20884 986 79722509
Drug abuse 23.01 16.60 7 20886 162684 79560811
Disseminated tuberculosis 22.76 16.60 14 20879 4169 79719326
Pubertal failure 22.76 16.60 4 20889 15 79723480
Ovarian failure 22.66 16.60 8 20885 668 79722827
Pre-eclampsia 22.61 16.60 17 20876 7024 79716471
Erythema elevatum diutinum 22.56 16.60 4 20889 16 79723479
Meningitis tuberculous 21.47 16.60 9 20884 1196 79722299
Oral candidiasis 21.10 16.60 32 20861 29596 79693899
Social avoidant behaviour 20.96 16.60 14 20879 4800 79718695
Confusional state 20.76 16.60 32 20861 317965 79405530
Discomfort 20.50 16.60 4 20889 125613 79597882
Inappropriate schedule of product administration 20.30 16.60 5 20888 133623 79589872
CD4 lymphocytes increased 20.13 16.60 6 20887 292 79723203
Breech delivery 20.10 16.60 4 20889 33 79723462
Crystal urine 19.94 16.60 5 20888 126 79723369
Tuberculoma of central nervous system 19.88 16.60 7 20886 580 79722915
Post transplant distal limb syndrome 19.73 16.60 7 20886 593 79722902
Nephropathy 19.73 16.60 18 20875 9720 79713775
5'nucleotidase increased 19.66 16.60 3 20890 3 79723492
Stomatitis 19.55 16.60 7 20886 146750 79576745
Injection site pain 19.45 16.60 5 20888 129833 79593662
Caesarean section 19.42 16.60 20 20873 12515 79710980
Epistaxis 19.41 16.60 3 20890 111512 79611983
Ocular icterus 19.28 16.60 14 20879 5486 79718009
Polydipsia 19.13 16.60 15 20878 6590 79716905
Generalised anxiety disorder 19.13 16.60 10 20883 2187 79721308
Weight increased 18.99 16.60 27 20866 277359 79446136
Antiviral drug level below therapeutic 18.90 16.60 4 20889 46 79723449
Hepatomegaly 18.87 16.60 24 20869 18850 79704645
Infertility 18.67 16.60 7 20886 694 79722801
Myocardial infarction 18.36 16.60 96 20797 184033 79539462
Chronic kidney disease 18.25 16.60 48 20845 66106 79657389
Hepatosplenomegaly 18.05 16.60 14 20879 6055 79717440
Arthritis 18.04 16.60 4 20889 114876 79608619
Aspartate aminotransferase increased 17.98 16.60 78 20815 138563 79584932
Trimethylaminuria 17.94 16.60 5 20888 191 79723304
Maternal exposure during pregnancy 17.84 16.60 77 20816 136461 79587034
Diabetes mellitus 17.81 16.60 53 20840 78337 79645158
Musculoskeletal stiffness 17.79 16.60 12 20881 174996 79548499
Alanine aminotransferase increased 17.78 16.60 87 20806 162483 79561012
Mobility decreased 17.74 16.60 5 20888 122170 79601325
Infected vasculitis 17.59 16.60 3 20890 9 79723486
Ear malformation 17.59 16.60 3 20890 9 79723486
Oligohydramnios 17.51 16.60 11 20882 3401 79720094
Subchondral insufficiency fracture 17.50 16.60 4 20889 67 79723428
Fatigue 17.37 16.60 158 20735 929569 78793926
Febrile neutropenia 17.33 16.60 21 20872 230978 79492517
Hepatic function abnormal 17.15 16.60 50 20843 73057 79650438
Hepatitis 17.00 16.60 42 20851 55685 79667810
Liver function test abnormal 16.99 16.60 46 20847 64429 79659066
Dizziness 16.72 16.60 76 20817 526365 79197130
Cellulitis 16.72 16.60 4 20889 109056 79614439

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
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 D019384 Nucleic Acid Synthesis Inhibitors
MeSH PA D018894 Reverse Transcriptase Inhibitors
CHEBI has role CHEBI:36044 antiviral drugs
CHEBI has role CHEBI:53756 reverse transcriptase inhibitors
CHEBI has role CHEBI:88188 allergenic drug
FDA MoA N0000193954 Cytochrome P450 1A1 Inhibitors

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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ 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
168146-84-7 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
CHEMBL1200619 ChEMBL_ID
C106538 MESH_SUPPLEMENTAL_RECORD_UI
441300 PUBCHEM_CID
11152 IUPHAR_LIGAND_ID
7544 INN_ID
WR2TIP26VS UNII
116084008 SNOMEDCT_US
387005008 SNOMEDCT_US
412074007 SNOMEDCT_US
4021139 VANDF
4024130 VANDF
4029879 VANDF
14010 MMSL
191490 MMSL
30504 MMSL
66957 MMSL
7865 MMSL
d04376 MMSL
007687 NDDF
007688 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Abacavir HUMAN PRESCRIPTION DRUG LABEL 1 0121-0897 SOLUTION 20 mg ORAL ANDA 28 sections
Abacavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0378-4105 TABLET, FILM COATED 300 mg ORAL ANDA 28 sections
Abacavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0904-6523 TABLET, FILM COATED 300 mg ORAL ANDA 28 sections
Abacavir HUMAN PRESCRIPTION DRUG LABEL 1 0904-6874 TABLET, FILM COATED 300 mg ORAL ANDA 28 sections
Abacavir Human Prescription Drug Label 1 31722-557 TABLET 300 mg ORAL ANDA 27 sections
Abacavir Human Prescription Drug Label 1 31722-562 SOLUTION 20 mg ORAL ANDA 28 sections
Abacavir and Lamivudine Human Prescription Drug Label 2 35573-402 TABLET, FILM COATED 600 mg ORAL ANDA 29 sections
Abacavir and Lamivudine Human Prescription Drug Label 2 35573-430 TABLET, FILM COATED 600 mg ORAL ANDA 27 sections
Abacavir and Lamivudine Human Prescription Drug Label 2 35573-430 TABLET, FILM COATED 600 mg ORAL ANDA 27 sections
Abacavir and Lamivudine HUMAN PRESCRIPTION DRUG LABEL 2 42291-115 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
Abacavir and Lamivudine Human Prescription Drug Label 2 42385-962 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
EPZICOM HUMAN PRESCRIPTION DRUG LABEL 2 49702-206 TABLET, FILM COATED 600 mg ORAL NDA 27 sections
EPZICOM HUMAN PRESCRIPTION DRUG LABEL 2 49702-206 TABLET, FILM COATED 600 mg ORAL NDA 27 sections
EPZICOM HUMAN PRESCRIPTION DRUG LABEL 2 49702-206 TABLET, FILM COATED 600 mg ORAL NDA 27 sections
TRIZIVIR HUMAN PRESCRIPTION DRUG LABEL 3 49702-217 TABLET, FILM COATED 300 mg ORAL NDA 26 sections
TRIZIVIR HUMAN PRESCRIPTION DRUG LABEL 3 49702-217 TABLET, FILM COATED 300 mg ORAL NDA 26 sections
TRIZIVIR HUMAN PRESCRIPTION DRUG LABEL 3 49702-217 TABLET, FILM COATED 300 mg ORAL NDA 26 sections
ZIAGEN HUMAN PRESCRIPTION DRUG LABEL 1 49702-221 TABLET, FILM COATED 300 mg ORAL NDA 26 sections
ZIAGEN HUMAN PRESCRIPTION DRUG LABEL 1 49702-221 TABLET, FILM COATED 300 mg ORAL NDA 26 sections
ZIAGEN HUMAN PRESCRIPTION DRUG LABEL 1 49702-221 TABLET, FILM COATED 300 mg ORAL NDA 26 sections
ZIAGEN HUMAN PRESCRIPTION DRUG LABEL 1 49702-222 SOLUTION 20 mg ORAL NDA 26 sections
ZIAGEN HUMAN PRESCRIPTION DRUG LABEL 1 49702-222 SOLUTION 20 mg ORAL NDA 26 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
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 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 29 sections