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

Stem definitionDrug idCAS RN
antivirals 989 154598-52-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • efavirenz
  • stocrin
  • (-)-Efavirenz
  • sustiva
Efavirenz is a non-nucleoside reverse transcriptase (RT) inhibitor of HIV-1. Efavirenz activity is mediated predominantly by noncompetitive inhibition of HIV-1 reverse transcriptase. HIV-2 RT and human cellular DNA polymerases alpha, beta, gamma, and delta are not inhibited by efavirenz.
  • Molecular weight: 315.68
  • Formula: C14H9ClF3NO2
  • CLOGP: 3.92
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 38.33
  • ALOGS: -4.57
  • ROTB: 3

  • 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) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.01 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 27.15 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 42.50 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Sept. 17, 1998 FDA BRISTOL MYERS SQUIBB

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
Abortion spontaneous 642.33 25.03 248 8403 41524 50554949
Viral mutation identified 560.66 25.03 112 8539 1517 50594956
Maternal exposure during pregnancy 555.50 25.03 342 8309 159436 50437037
Virologic failure 505.17 25.03 102 8549 1462 50595011
Pregnancy 434.22 25.03 170 8481 29407 50567066
Abortion induced 426.86 25.03 126 8525 9218 50587255
Immune reconstitution inflammatory syndrome 386.68 25.03 104 8547 5412 50591061
Exposure during pregnancy 374.24 25.03 241 8410 120774 50475699
Stillbirth 374.21 25.03 103 8548 5849 50590624
Drug resistance 299.23 25.03 115 8536 18874 50577599
Normal newborn 261.32 25.03 80 8571 6611 50589862
Pathogen resistance 260.93 25.03 77 8574 5612 50590861
Foetal exposure during pregnancy 233.21 25.03 107 8544 27252 50569221
Blood HIV RNA increased 172.41 25.03 35 8616 514 50595959
Lipodystrophy acquired 167.15 25.03 40 8611 1289 50595184
Live birth 151.84 25.03 68 8583 16340 50580133
Caesarean section 126.41 25.03 59 8592 15580 50580893
Premature delivery 108.75 25.03 61 8590 23602 50572871
Birth mark 94.90 25.03 17 8634 121 50596352
Viral load increased 91.27 25.03 24 8627 1139 50595334
Cerebellar ataxia 87.90 25.03 22 8629 856 50595617
Lactic acidosis 87.08 25.03 60 8591 33295 50563178
Pregnancy with implant contraceptive 86.70 25.03 26 8625 1997 50594476
Congenital umbilical hernia 81.01 25.03 17 8634 296 50596177
Pregnancy on contraceptive 79.17 25.03 21 8630 1031 50595442
Pulmonary tuberculosis 78.54 25.03 29 8622 4244 50592229
Treatment noncompliance 68.88 25.03 50 8601 30100 50566373
Fanconi syndrome acquired 67.44 25.03 18 8633 905 50595568
Ectopic pregnancy 54.88 25.03 19 8632 2308 50594165
Cleft lip and palate 51.25 25.03 12 8639 351 50596122
Hepatitis fulminant 49.75 25.03 19 8632 3049 50593424
Foetal death 48.52 25.03 25 8626 8155 50588318
CD4 lymphocytes decreased 47.98 25.03 15 8636 1324 50595149
Portal hypertension 47.90 25.03 19 8632 3373 50593100
Autoimmune hepatitis 47.56 25.03 24 8627 7495 50588978
Drug interaction 47.43 25.03 105 8546 199516 50396957
Immune reconstitution inflammatory syndrome associated tuberculosis 47 25.03 11 8640 321 50596152
Tuberculosis 46.31 25.03 26 8625 10057 50586416
Malaria 46.24 25.03 10 8641 202 50596271
Cholestatic liver injury 45.73 25.03 16 8635 2005 50594468
Premature baby 45.53 25.03 32 8619 18305 50578168
Pain 42.74 25.03 23 8628 578880 50017593
Fatigue 40.55 25.03 37 8614 707564 49888909
Nephropathy toxic 40.43 25.03 22 8629 8007 50588466
Hepatomegaly 39.45 25.03 24 8627 10769 50585704
Premature rupture of membranes 39.23 25.03 18 8633 4562 50591911
Rash maculo-papular 36.96 25.03 33 8618 26608 50569865
Anaemia 35.40 25.03 109 8542 252347 50344126
Congenital anomaly 34.25 25.03 12 8639 1509 50594964
Twin pregnancy 33.83 25.03 11 8640 1102 50595371
Gene mutation 32.39 25.03 11 8640 1260 50595213
Cardiac malposition 32.24 25.03 6 8645 54 50596419
Maternal drugs affecting foetus 31.51 25.03 16 8635 5061 50591412
Spinocerebellar disorder 31.44 25.03 5 8646 15 50596458
Pregnancy on oral contraceptive 31.29 25.03 10 8641 948 50595525
Pachygyria 30.70 25.03 4 8647 0 50596473
Drug ineffective 30.44 25.03 59 8592 819274 49777199
Arthralgia 30.09 25.03 19 8632 438683 50157790
Pre-eclampsia 29.68 25.03 18 8633 8026 50588447
Meningitis cryptococcal 29.54 25.03 10 8641 1135 50595338
Retinal toxicity 29.18 25.03 10 8641 1178 50595295
Hepatic displacement 29.10 25.03 5 8646 27 50596446
Diastasis recti abdominis 27.74 25.03 5 8646 37 50596436
Jaundice 27.63 25.03 28 8623 26401 50570072
HIV-associated neurocognitive disorder 27.57 25.03 6 8645 125 50596348
Isosporiasis 27.39 25.03 5 8646 40 50596433
Polydactyly 27.22 25.03 7 8644 304 50596169
Lipoatrophy 27.17 25.03 7 8644 306 50596167
Cytomegalovirus chorioretinitis 26.85 25.03 10 8641 1497 50594976
AIDS related complication 26.65 25.03 4 8647 7 50596466
Hydrocephalus 26.58 25.03 14 8637 4774 50591699
Type III hyperlipidaemia 26.31 25.03 4 8647 8 50596465
Renal tubular disorder 25.43 25.03 11 8640 2426 50594047
Multiple-drug resistance 25.21 25.03 12 8639 3302 50593171

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
Depression 1116.33 16.25 675 17441 84472 29471939
Immune reconstitution inflammatory syndrome 825.95 16.25 270 17846 7532 29548879
Drug interaction 754.54 16.25 752 17364 196633 29359778
Virologic failure 703.99 16.25 190 17926 2657 29553754
Viral mutation identified 676.52 16.25 179 17937 2309 29554102
Lipodystrophy acquired 574.62 16.25 165 17951 2929 29553482
Pathogen resistance 489.95 16.25 185 17931 7931 29548480
Mitochondrial toxicity 285.70 16.25 91 18025 2320 29554091
Progressive external ophthalmoplegia 230.03 16.25 67 18049 1250 29555161
Drug resistance 223.48 16.25 148 17968 21392 29535019
Loss of personal independence in daily activities 214.89 16.25 154 17962 25286 29531125
Eyelid ptosis 201.04 16.25 86 18030 5100 29551311
Lipoatrophy 151.24 16.25 39 18077 450 29555961
Foetal exposure during pregnancy 140.84 16.25 136 17980 33731 29522680
Psychiatric decompensation 127.08 16.25 44 18072 1460 29554951
CD4 lymphocytes decreased 120.68 16.25 43 18073 1555 29554856
Diplopia 114.44 16.25 82 18034 13436 29542975
Abnormal dreams 111.36 16.25 63 18053 6857 29549554
Depression suicidal 109.29 16.25 38 18078 1277 29555134
Tearfulness 104.84 16.25 39 18077 1597 29554814
Pulmonary tuberculosis 99.71 16.25 50 18066 4265 29552146
Retinal toxicity 95.28 16.25 26 18090 378 29556033
Treatment failure 94.83 16.25 115 18001 36824 29519587
Hyperlipidaemia 94.44 16.25 71 18045 12519 29543892
Blood HIV RNA increased 82.83 16.25 29 18087 995 29555416
Viral load increased 82.77 16.25 35 18081 2014 29554397
Paranoia 79.23 16.25 58 18058 9819 29546592
Hyperlactacidaemia 73.79 16.25 35 18081 2643 29553768
Kaposi's sarcoma 71.98 16.25 25 18091 837 29555574
Gynaecomastia 69.89 16.25 50 18066 8167 29548244
Fanconi syndrome acquired 69.57 16.25 30 18086 1812 29554599
Off label use 69.54 16.25 50 18066 300750 29255661
Hepatic fibrosis 67.34 16.25 35 18081 3217 29553194
Renal tubular disorder 63.02 16.25 37 18079 4315 29552096
Ophthalmoplegia 62.23 16.25 27 18089 1655 29554756
Depressive symptom 58.47 16.25 26 18090 1691 29554720
Fanconi syndrome 57.00 16.25 25 18091 1573 29554838
Treatment noncompliance 56.64 16.25 72 18044 24155 29532256
HIV-associated neurocognitive disorder 54.69 16.25 16 18100 303 29556108
Meningitis cryptococcal 53.47 16.25 26 18090 2074 29554337
Hypertriglyceridaemia 51.31 16.25 40 18076 7435 29548976
Psychomotor skills impaired 47.65 16.25 26 18090 2635 29553776
Immune reconstitution inflammatory syndrome associated tuberculosis 46.57 16.25 15 18101 396 29556015
Death 46.49 16.25 87 18029 341997 29214414
Psychotic disorder 45.24 16.25 59 18057 20295 29536116
Pneumonia 44.76 16.25 80 18036 320092 29236319
Multiple-drug resistance 43.33 16.25 28 18088 3872 29552539
Nephropathy toxic 42.42 16.25 42 18074 10714 29545697
Osteoporosis 40.54 16.25 41 18075 10728 29545683
Fall 40.13 16.25 30 18086 177148 29379263
Hepatitis 39.74 16.25 56 18060 20727 29535684
Portal hypertension 38.66 16.25 25 18091 3461 29552950
Nightmare 38.54 16.25 41 18075 11376 29545035
Retroviral rebound syndrome 38.19 16.25 7 18109 11 29556400
Febrile neutropenia 37.69 16.25 11 18105 112229 29444182
Drug abuse 37.62 16.25 3 18113 79880 29476531
Lymph node tuberculosis 37.55 16.25 13 18103 431 29555980
Hydrocele 37.54 16.25 20 18096 1933 29554478
Dyslipidaemia 36.42 16.25 30 18086 6031 29550380
Renal impairment 36.33 16.25 121 17995 81212 29475199
Tuberculosis 35.86 16.25 32 18084 7164 29549247
Lymphadenopathy 35.86 16.25 59 18057 24990 29531421
Hypotension 35.60 16.25 40 18076 194314 29362097
Proteinuria 35.41 16.25 46 18070 15758 29540653
Drug ineffective 35.34 16.25 110 18006 363060 29193351
Fatigue 35.22 16.25 90 18026 316731 29239680
Lactic acidosis 35.17 16.25 65 18051 30182 29526229
Tuberculoid leprosy 34.34 16.25 8 18108 58 29556353
Product dose omission issue 33.18 16.25 9 18107 96374 29460037
Pain 32.81 16.25 34 18082 171398 29385013
Atrial fibrillation 32.57 16.25 12 18104 105634 29450777
Neurosyphilis 32.11 16.25 7 18109 36 29556375
Mycobacterium avium complex infection 32.09 16.25 19 18097 2250 29554161
Blood triglycerides increased 31.35 16.25 39 18077 12795 29543616
HIV infection 31.21 16.25 15 18101 1166 29555245
Developmental hip dysplasia 30.45 16.25 10 18106 281 29556130
Constipation 30.41 16.25 16 18100 114144 29442267
Drug-induced liver injury 29.65 16.25 50 18066 21605 29534806
Hypophosphataemia 29.51 16.25 30 18086 7894 29548517
Cryptococcosis 29.33 16.25 17 18099 1935 29554476
Cachexia 29.22 16.25 27 18089 6322 29550089
Suicidal ideation 28.94 16.25 65 18051 34651 29521760
Nervous system disorder 28.56 16.25 37 18079 12637 29543774
Hepatosplenomegaly 27.94 16.25 21 18095 3696 29552715
Mycobacterium avium complex immune restoration disease 27.83 16.25 6 18110 29 29556382
Hepatic cirrhosis 27.73 16.25 39 18077 14405 29542006
Blood lactic acid increased 27.47 16.25 25 18091 5741 29550670
Hepatomegaly 27.19 16.25 31 18085 9286 29547125
Genotype drug resistance test positive 27.05 16.25 13 18103 1010 29555401
Vanishing bile duct syndrome 26.97 16.25 11 18105 577 29555834
Intracranial pressure increased 26.89 16.25 20 18096 3465 29552946
Acquired immunodeficiency syndrome 26.70 16.25 10 18106 417 29555994
Osteonecrosis 26.69 16.25 37 18079 13482 29542929
Megakaryocytes increased 26.46 16.25 6 18110 38 29556373
Congenital umbilical hernia 26.42 16.25 9 18107 284 29556127
Mitochondrial cytopathy 26.34 16.25 8 18108 173 29556238
Histoplasmosis disseminated 25.67 16.25 13 18103 1131 29555280
Hepatotoxicity 25.45 16.25 42 18074 17825 29538586
Blood pressure increased 25.19 16.25 7 18109 73796 29482615
Psychomotor retardation 25.05 16.25 18 18098 2958 29553453
Aspartate aminotransferase increased 25.02 16.25 87 18029 59638 29496773
Infection 24.89 16.25 8 18108 76743 29479668
Night blindness 24.77 16.25 8 18108 213 29556198
Hepatitis B 24.57 16.25 23 18093 5474 29550937
Dyspnoea 24.53 16.25 110 18006 326622 29229789
Liver transplant 24.19 16.25 16 18100 2300 29554111
Sickle cell disease 23.95 16.25 7 18109 132 29556279
Oral candidiasis 23.69 16.25 31 18085 10691 29545720
Renal tubular dysfunction 23.40 16.25 9 18107 404 29556007
Toxoplasma serology positive 23.36 16.25 4 18112 3 29556408
Hepatitis C 23.26 16.25 28 18088 8882 29547529
Meningitis tuberculous 23.01 16.25 10 18106 615 29555796
Renal tubular acidosis 22.67 16.25 14 18102 1789 29554622
Back pain 22.26 16.25 18 18098 102266 29454145
Nodular regenerative hyperplasia 22.16 16.25 10 18106 673 29555738
Limb deformity 21.56 16.25 9 18107 501 29555910
Cytomegalovirus chorioretinitis 21.51 16.25 17 18099 3221 29553190
Product use issue 21.48 16.25 3 18113 51441 29504970
Mitochondrial myopathy 21.31 16.25 7 18109 197 29556214
Synostosis 21.00 16.25 6 18110 104 29556307
Hypercholesterolaemia 20.98 16.25 24 18092 7214 29549197
Polyneuropathy chronic 20.92 16.25 5 18111 41 29556370
Anal cancer 20.87 16.25 8 18108 356 29556055
Lipohypertrophy 20.85 16.25 7 18109 211 29556200
Talipes 20.23 16.25 13 18103 1779 29554632
Gamma-glutamyltransferase increased 20.02 16.25 48 18068 26689 29529722
Congenital eyelid malformation 19.95 16.25 5 18111 51 29556360
Glycosuria 19.83 16.25 11 18105 1151 29555260
Platelet count decreased 19.73 16.25 21 18095 104651 29451760
Amylase increased 19.68 16.25 20 18096 5260 29551151
Tubulointerstitial nephritis 19.36 16.25 37 18079 17606 29538805
Korsakoff's syndrome 19.20 16.25 3 18113 0 29556411
Osteoporotic fracture 18.63 16.25 10 18106 981 29555430
Birth mark 18.46 16.25 6 18110 163 29556248
Nephrolithiasis 18.45 16.25 45 18071 25289 29531122
Elbow synostosis 18.44 16.25 4 18112 20 29556391
Liver injury 18.30 16.25 30 18086 12660 29543751
Neck deformity 18.30 16.25 5 18111 73 29556338
Subacute sclerosing panencephalitis 18.28 16.25 4 18112 21 29556390
Nasopharyngitis 18.00 16.25 7 18109 59658 29496753
Congenital tuberculosis 17.83 16.25 4 18112 24 29556387
Alanine aminotransferase increased 17.60 16.25 88 18028 70856 29485555
Trisomy 18 17.59 16.25 6 18110 190 29556221
Congenital bowing of long bones 17.42 16.25 4 18112 27 29556384
Castleman's disease 17.42 16.25 4 18112 27 29556384
Eyelid ptosis congenital 17.22 16.25 5 18111 92 29556319
Hepatic function abnormal 17.14 16.25 58 18058 39201 29517210
Oesophageal candidiasis 17.10 16.25 16 18100 3805 29552606
Pneumocystis jirovecii pneumonia 16.97 16.25 34 18082 16745 29539666
Osteomalacia 16.92 16.25 9 18107 867 29555544
Meconium ileus 16.83 16.25 4 18112 32 29556379
Protein S deficiency 16.74 16.25 5 18111 102 29556309
Pulmonary oedema 16.69 16.25 3 18113 42732 29513679
Fibrous histiocytoma 16.51 16.25 5 18111 107 29556304
Hydrops foetalis 16.40 16.25 6 18110 234 29556177

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
Immune reconstitution inflammatory syndrome 1240.13 15.77 355 20589 12115 64465673
Lipodystrophy acquired 688.84 15.77 176 20768 3851 64473937
Virologic failure 674.76 15.77 168 20776 3298 64474490
Depression 673.95 15.77 521 20423 182770 64295018
Viral mutation identified 670.55 15.77 166 20778 3180 64474608
Drug interaction 548.07 15.77 628 20316 361455 64116333
Drug resistance 494.82 15.77 237 20707 34865 64442923
Abortion spontaneous 354.91 15.77 170 20774 24973 64452815
Mitochondrial toxicity 346.31 15.77 94 20850 2612 64475176
Pathogen resistance 321.20 15.77 129 20815 12414 64465374
Abortion induced 317.26 15.77 107 20837 6281 64471507
Progressive external ophthalmoplegia 271.66 15.77 67 20877 1260 64476528
Stillbirth 246.07 15.77 77 20867 3556 64474232
Blood HIV RNA increased 215.63 15.77 57 20887 1427 64476361
Maternal exposure during pregnancy 209.44 15.77 203 20741 95681 64382107
Pregnancy 206.42 15.77 111 20833 20754 64457034
Pulmonary tuberculosis 190.61 15.77 76 20868 7168 64470620
Eyelid ptosis 190.00 15.77 82 20862 9443 64468345
Exposure during pregnancy 187.80 15.77 174 20770 77501 64400287
CD4 lymphocytes decreased 162.35 15.77 51 20893 2384 64475404
Loss of personal independence in daily activities 161.16 15.77 155 20789 72299 64405489
Lipoatrophy 154.69 15.77 37 20907 608 64477180
Psychiatric decompensation 133.18 15.77 44 20900 2419 64475369
Retinal toxicity 128.13 15.77 37 20907 1293 64476495
Fanconi syndrome acquired 118.00 15.77 40 20904 2381 64475407
Depression suicidal 117.14 15.77 40 20904 2435 64475353
Viral load increased 113.06 15.77 39 20905 2448 64475340
Tearfulness 109.10 15.77 45 20899 4628 64473160
Diplopia 108.62 15.77 81 20863 26684 64451104
Lactic acidosis 101.42 15.77 112 20832 61298 64416490
Meningitis cryptococcal 98.47 15.77 37 20907 2972 64474816
Immune reconstitution inflammatory syndrome associated tuberculosis 94.92 15.77 26 20918 747 64477041
Caesarean section 89.70 15.77 52 20892 11222 64466566
Nephropathy toxic 87.13 15.77 60 20884 17454 64460334
Gynaecomastia 85.79 15.77 41 20903 5975 64471813
Normal newborn 85.37 15.77 40 20904 5577 64472211
Paranoia 83.66 15.77 57 20887 16295 64461493
Pain 81.62 15.77 39 20905 553472 63924316
Treatment noncompliance 80.03 15.77 84 20860 43398 64434390
Portal hypertension 78.52 15.77 39 20905 6180 64471608
Tuberculosis 77.73 15.77 50 20894 12988 64464800
Multiple-drug resistance 76.88 15.77 39 20905 6463 64471325
Hepatic fibrosis 76.63 15.77 37 20907 5515 64472273
Abnormal dreams 75.13 15.77 45 20899 10311 64467477
Pregnancy on contraceptive 71.75 15.77 21 20923 770 64477018
HIV-associated neurocognitive disorder 69.45 15.77 17 20927 309 64477479
Fanconi syndrome 68.44 15.77 27 20917 2474 64475314
Renal tubular disorder 68.14 15.77 35 20909 5952 64471836
Live birth 66.87 15.77 43 20901 11161 64466627
Hyperlipidaemia 66.42 15.77 57 20887 22919 64454869
Hepatomegaly 63.86 15.77 49 20895 16833 64460955
Hyperlactacidaemia 63.01 15.77 31 20913 4813 64472975
Ophthalmoplegia 63.00 15.77 26 20918 2676 64475112
Lymph node tuberculosis 59.49 15.77 19 20925 937 64476851
Psychotic disorder 58.68 15.77 64 20880 34514 64443274
Nightmare 56.49 15.77 50 20894 20943 64456845
Pregnancy with implant contraceptive 55.27 15.77 20 20924 1444 64476344
Off label use 54.30 15.77 76 20868 632730 63845058
Psychomotor skills impaired 54.20 15.77 26 20918 3819 64473969
Mycobacterium avium complex infection 53.60 15.77 26 20918 3914 64473874
Lymphadenopathy 50.80 15.77 69 20875 46617 64431171
Depressive symptom 50.35 15.77 26 20918 4470 64473318
Hypertriglyceridaemia 50.17 15.77 36 20908 11169 64466619
Joint swelling 49.30 15.77 6 20938 215376 64262412
Fatigue 48.75 15.77 107 20837 748623 63729165
Kaposi's sarcoma 47.08 15.77 15 20929 734 64477054
Cachexia 46.84 15.77 32 20912 9185 64468603
Cholestatic liver injury 46.23 15.77 23 20921 3656 64474132
Drug ineffective 46.22 15.77 131 20813 840116 63637672
Hepatitis 46.04 15.77 65 20879 45517 64432271
Nasopharyngitis 46.03 15.77 5 20939 196068 64281720
Fall 45.60 15.77 41 20903 416785 64061003
Drug-induced liver injury 45.28 15.77 66 20878 47577 64430211
Dyslipidaemia 44.41 15.77 31 20913 9211 64468577
Hepatic cirrhosis 43.45 15.77 48 20896 26250 64451538
Cytomegalovirus chorioretinitis 42.68 15.77 24 20920 4888 64472900
Megakaryocytes increased 42.12 15.77 9 20935 86 64477702
Rheumatoid arthritis 41.78 15.77 3 20941 164291 64313497
Meningitis tuberculous 41.28 15.77 15 20929 1096 64476692
Tuberculoid leprosy 40.64 15.77 9 20935 103 64477685
Anaemia 39.82 15.77 234 20710 378446 64099342
Ectopic pregnancy 39.72 15.77 16 20928 1548 64476240
Blood triglycerides increased 39.34 15.77 39 20905 18827 64458961
Product dose omission issue 38.77 15.77 8 20936 194739 64283049
Genotype drug resistance test positive 38.44 15.77 14 20930 1030 64476758
Premature delivery 37.97 15.77 38 20906 18551 64459237
Hypophosphataemia 37.51 15.77 34 20910 14686 64463102
Aplasia pure red cell 37.18 15.77 25 20919 6989 64470799
Cryptococcosis 36.93 15.77 18 20926 2737 64475051
Night blindness 36.56 15.77 11 20933 444 64477344
Hypercholesterolaemia 36.24 15.77 34 20910 15339 64462449
Infection 35.98 15.77 8 20936 184872 64292916
Renal tubular dysfunction 35.83 15.77 12 20932 688 64477100
Osteomalacia 34.53 15.77 14 20930 1377 64476411
Tuberculoma of central nervous system 34.43 15.77 11 20933 543 64477245
Aspartate aminotransferase increased 34.36 15.77 101 20843 119687 64358101
Malaria 34.21 15.77 10 20934 365 64477423
Renal impairment 33.31 15.77 108 20836 134909 64342879
Disseminated tuberculosis 32.18 15.77 18 20926 3627 64474161
Hepatotoxicity 31.81 15.77 51 20893 39911 64437877
Proteinuria 31.72 15.77 42 20902 27681 64450107
Pain in extremity 31.71 15.77 31 20913 303054 64174734
Dyspnoea 31.25 15.77 124 20820 718550 63759238
Sinusitis 31.18 15.77 5 20939 145923 64331865
Autoimmune hepatitis 31.16 15.77 26 20918 10058 64467730
Constipation 30.99 15.77 18 20926 229319 64248469
Pneumonia 30.85 15.77 87 20857 559489 63918299
Jaundice 30.82 15.77 56 20888 48456 64429332
Hepatosplenomegaly 30.64 15.77 20 20924 5323 64472465
Arthralgia 30.54 15.77 61 20883 442199 64035589
Low density lipoprotein increased 30.44 15.77 23 20921 7717 64470071
Hepatitis B 30.43 15.77 23 20921 7722 64470066
Intracranial pressure increased 30.25 15.77 22 20922 6967 64470821
Extrapulmonary tuberculosis 29.80 15.77 9 20935 368 64477420
Abdominal discomfort 29.75 15.77 11 20933 182311 64295477
Nervous system disorder 29.60 15.77 37 20907 23041 64454747
Nodular regenerative hyperplasia 29.57 15.77 11 20933 859 64476929
Febrile neutropenia 29.49 15.77 12 20932 187645 64290143
Mitochondrial cytopathy 29.43 15.77 9 20935 384 64477404
Oral candidiasis 29.43 15.77 37 20907 23175 64454613
Back pain 29.29 15.77 23 20921 250148 64227640
Swelling 29.09 15.77 8 20936 160210 64317578
Retroviral rebound syndrome 29.05 15.77 5 20939 12 64477776
Pneumocystis jirovecii pneumonia 28.78 15.77 40 20904 27594 64450194
Gamma-glutamyltransferase increased 28.32 15.77 54 20890 48456 64429332
HIV infection 28.27 15.77 11 20933 971 64476817
Suicidal ideation 28.24 15.77 65 20879 66477 64411311
Hepatitis fulminant 27.73 15.77 20 20924 6254 64471534
Pregnancy on oral contraceptive 27.13 15.77 10 20934 761 64477027
Renal tubular acidosis 27.09 15.77 15 20929 2964 64474824
Mycobacterium avium complex immune restoration disease 26.93 15.77 5 20939 21 64477767
Therapeutic product effect decreased 26.91 15.77 3 20941 115348 64362440
Atrial fibrillation 26.79 15.77 11 20933 171078 64306710
Neurosyphilis 26.38 15.77 5 20939 24 64477764
Alanine aminotransferase increased 26.36 15.77 102 20842 138929 64338859
Gene mutation 26.11 15.77 13 20931 2069 64475719
Rash maculo-papular 25.80 15.77 51 20893 46975 64430813
Injection site pain 25.73 15.77 3 20941 111405 64366383
Vanishing bile duct syndrome 25.48 15.77 11 20933 1266 64476522
Oesophageal candidiasis 25.45 15.77 21 20923 7996 64469792
Liver transplant 25.15 15.77 16 20928 4076 64473712
Cerebral toxoplasmosis 24.69 15.77 12 20932 1814 64475974
Rash scarlatiniform 24.68 15.77 7 20937 229 64477559
Hepatic necrosis 24.44 15.77 21 20923 8452 64469336
Psychomotor retardation 24.12 15.77 17 20927 5126 64472662
Blood pressure increased 24.08 15.77 13 20931 172539 64305249
Transaminases increased 24.03 15.77 48 20896 44546 64433242
Arthropathy 24.00 15.77 5 20939 120962 64356826
Type III hyperlipidaemia 23.74 15.77 4 20940 8 64477780
Hypotension 23.44 15.77 56 20888 380918 64096870
Hepatitis C 23.39 15.77 23 20921 10992 64466796
Central nervous system immune reconstitution inflammatory response 23.28 15.77 5 20939 49 64477739
Mitochondrial myopathy 23.28 15.77 7 20937 282 64477506
Pyrexia 23.18 15.77 280 20664 558364 63919424
Red blood cell abnormality 22.81 15.77 8 20936 527 64477261
AIDS related complication 22.60 15.77 5 20939 57 64477731
Haemophagocytic lymphohistiocytosis 22.21 15.77 28 20916 17581 64460207
Influenza 21.99 15.77 4 20940 106527 64371261
CD4 lymphocytes 21.70 15.77 4 20940 16 64477772
Premature rupture of membranes 21.43 15.77 14 20930 3730 64474058
Completed suicide 21.18 15.77 25 20919 224389 64253399
Therapeutic product effect incomplete 21.11 15.77 4 20940 103478 64374310
Musculoskeletal stiffness 20.83 15.77 7 20937 123199 64354589
Bronchitis 20.56 15.77 5 20939 108738 64369050
Acquired immunodeficiency syndrome 20.55 15.77 6 20938 218 64477570
Glycosuria 20.40 15.77 11 20933 2063 64475725
Viral load decreased 20.36 15.77 4 20940 24 64477764
Nausea 20.24 15.77 161 20783 785639 63692149
Amylase increased 20.15 15.77 20 20924 9665 64468123
Osteoporosis 19.98 15.77 43 20901 42037 64435751
Hepatic steatosis 19.95 15.77 36 20908 30971 64446817
Cerebellar syndrome 19.94 15.77 15 20929 5001 64472787
Gait disturbance 19.92 15.77 16 20928 172139 64305649
Hepatic encephalopathy 19.74 15.77 29 20915 21037 64456751
Granulomatous liver disease 19.49 15.77 9 20935 1213 64476575
Anaemia macrocytic 19.39 15.77 14 20930 4384 64473404
Isosporiasis 19.35 15.77 5 20939 114 64477674
Twin pregnancy 19.24 15.77 8 20936 839 64476949
Visual field defect 19.17 15.77 18 20926 8128 64469660
Blood lactic acid increased 18.96 15.77 20 20924 10381 64467407
Weight increased 18.84 15.77 25 20919 213323 64264465
Subacute sclerosing panencephalitis 18.84 15.77 4 20940 37 64477751
Tubulointerstitial nephritis 18.77 15.77 35 20909 30874 64446914
Blood alkaline phosphatase increased 18.62 15.77 50 20894 56229 64421559
Hypertrophic cardiomyopathy 18.54 15.77 10 20934 1876 64475912
CSF HIV escape syndrome 18.35 15.77 6 20938 319 64477469
Cushingoid 18.28 15.77 17 20927 7586 64470202
Toxoplasma serology positive 18.12 15.77 4 20940 45 64477743
Acquired gene mutation 18.06 15.77 10 20934 1976 64475812
Histoplasmosis disseminated 18.00 15.77 10 20934 1988 64475800
Inappropriate schedule of product administration 17.93 15.77 4 20940 92282 64385506
Antiviral drug level above therapeutic 17.89 15.77 4 20940 48 64477740
Opportunistic infection 17.85 15.77 11 20933 2651 64475137
Foetal death 17.72 15.77 15 20929 5915 64471873
Oropharyngeal candidiasis 17.65 15.77 9 20935 1506 64476282
Encephalitis 17.49 15.77 21 20923 12550 64465238
Folate deficiency 17.47 15.77 11 20933 2752 64475036
Stevens-Johnson syndrome 17.42 15.77 36 20908 34213 64443575
Hepatic function abnormal 17.27 15.77 53 20891 64260 64413528
Liver disorder 17.25 15.77 47 20897 53304 64424484
Splenomegaly 17.23 15.77 25 20919 17936 64459852
Osteonecrosis 17.19 15.77 32 20912 28197 64449591
Acute stress disorder 17.08 15.77 6 20938 397 64477391
Myelitis transverse 17.07 15.77 9 20935 1614 64476174
Drug abuse 17.02 15.77 11 20933 132363 64345425
Nephrolithiasis 16.72 15.77 41 20903 43642 64434146
Drug intolerance 16.63 15.77 22 20922 187970 64289818
Viraemia 16.50 15.77 10 20934 2339 64475449
Colour vision tests abnormal 16.27 15.77 3 20941 12 64477776
Abdominal pain upper 15.98 15.77 20 20924 175010 64302778
Fat tissue increased 15.97 15.77 7 20937 836 64476952
Urinary tract infection 15.91 15.77 32 20912 231564 64246224
Pancreatitis 15.89 15.77 49 20895 59558 64418230

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AG03 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Non-nucleoside reverse transcriptase inhibitors
ATC J05AR06 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR11 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
FDA MoA N0000009948 Non-Nucleoside Reverse Transcriptase Inhibitors
FDA EXT N0000175460 Non-Nucleoside Analog
FDA EPC N0000175463 Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D065695 Cytochrome P-450 CYP2B6 Inducers
MeSH PA D065689 Cytochrome P-450 CYP2C19 Inhibitors
MeSH PA D065688 Cytochrome P-450 CYP2C9 Inhibitors
MeSH PA D065701 Cytochrome P-450 CYP3A Inducers
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances
MeSH PA D019384 Nucleic Acid Synthesis Inhibitors
MeSH PA D018894 Reverse Transcriptase Inhibitors
FDA MoA N0000182140 Cytochrome P450 2C19 Inhibitors
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000185504 Cytochrome P450 2C9 Inhibitors
FDA MoA N0000187064 Cytochrome P450 2B6 Inducers
FDA MoA N0000190118 Cytochrome P450 3A Inducers
CHEBI has role CHEBI:36044 antiviral drugs
CHEBI has role CHEBI:53756 reverse transcriptase inhibitors

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

DiseaseRelationSNOMED_IDDOID
Human immunodeficiency virus infection indication 86406008 DOID:526
Prevention of HIV Infection after Exposure off-label use
Osteomalacia contraindication 4598005 DOID:10573
Hypophosphatemia contraindication 4996001
Suicidal thoughts contraindication 6471006
Hypercholesterolemia contraindication 13644009
Depressive disorder contraindication 35489007
Fanconi syndrome contraindication 40488004 DOID:1062
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Aggressive behavior contraindication 61372001
Chronic type B viral hepatitis contraindication 61977001
Kidney disease contraindication 90708001 DOID:557
Lactic acidosis contraindication 91273001 DOID:3650
Chronic hepatitis C contraindication 128302006
Seizure disorder contraindication 128613002
Liver function tests abnormal contraindication 166603001
Paranoid disorder contraindication 191667009
Steatosis of liver contraindication 197321007
Mania contraindication 231494001
Disease of liver contraindication 235856003 DOID:409
Pathological fracture contraindication 268029009
Pregnancy, function contraindication 289908002
Hypertriglyceridemia contraindication 302870006
Osteopenia contraindication 312894000
Breastfeeding (mother) contraindication 413712001
Obesity contraindication 414916001 DOID:9970




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 10.6 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
600MG;200MG;300MG ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 RX TABLET ORAL 8592397 Jan. 13, 2024 TREATMENT OF HIV-1 INFECTION IN ADULTS
600MG;200MG;300MG ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 RX TABLET ORAL 8592397 Jan. 13, 2024 TREATMENT OF HIV-1 INFECTION IN PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER
600MG;200MG;300MG ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 RX TABLET ORAL 8716264 Jan. 13, 2024 TREATMENT OF HIV INFECTION
600MG;200MG;300MG ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 RX TABLET ORAL 9457036 Jan. 13, 2024 TREATMENT OF HIV INFECTION
600MG;200MG;300MG ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 RX TABLET ORAL 9744181 Jan. 13, 2024 TREATMENT OF HIV INFECTION
600MG;200MG;300MG ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 RX TABLET ORAL 9018192 June 13, 2026 TREATMENT OF HIV-1 INFECTION IN ADULTS
600MG;200MG;300MG ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 RX TABLET ORAL 9018192 June 13, 2026 TREATMENT OF HIV-1 INFECTION IN PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER
600MG;200MG;300MG ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 RX TABLET ORAL 9545414 June 13, 2026 TREATMENT OF HIV-1 INFECTION IN ADULTS
600MG;200MG;300MG ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 RX TABLET ORAL 9545414 June 13, 2026 TREATMENT OF HIV-1 INFECTION IN PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Nuclear receptor subfamily 1 group I member 2 Nuclear hormone receptor WOMBAT-PK
Cholesterol 24-hydroxylase Enzyme Kd 6.10 CHEMBL
Cytochrome P450 3A4 Enzyme INHIBITOR IC50 4.76 IUPHAR
Reverse transcriptase/RNaseH Enzyme INHIBITOR Ki 8.52 CHEMBL CHEMBL
Gag-Pol polyprotein Polyprotein INHIBITOR IC50 8.30 WOMBAT-PK
Reverse transcriptase Enzyme IC50 8.89 CHEMBL
Reverse transcriptase protein Unclassified Ki 8.07 CHEMBL
Envelope glycoprotein gp160 [Cleaved into: Surface protein gp120 Unclassified IC50 8.46 CHEMBL

External reference:

IDSource
4021133 VUID
N0000148587 NUI
D00896 KEGG_DRUG
4021133 VANDF
C0674428 UMLSCUI
CHEBI:119486 CHEBI
EFZ PDB_CHEM_ID
CHEMBL223228 ChEMBL_ID
DB00625 DRUGBANK_ID
C098320 MESH_SUPPLEMENTAL_RECORD_UI
64139 PUBCHEM_CID
11287 IUPHAR_LIGAND_ID
7718 INN_ID
JE6H2O27P8 UNII
195084 RXNORM
11884 MMSL
210786 MMSL
7492 MMSL
d04355 MMSL
007651 NDDF
116078005 SNOMEDCT_US
387001004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SUSTIVA HUMAN PRESCRIPTION DRUG LABEL 1 0056-0470 CAPSULE, GELATIN COATED 50 mg ORAL NDA 31 sections
SUSTIVA HUMAN PRESCRIPTION DRUG LABEL 1 0056-0474 CAPSULE, GELATIN COATED 200 mg ORAL NDA 31 sections
SUSTIVA HUMAN PRESCRIPTION DRUG LABEL 1 0056-0510 TABLET, FILM COATED 600 mg ORAL NDA 31 sections
Efavirenz, Emtricitabine and Tenofovir Disoproxil Fumarate HUMAN PRESCRIPTION DRUG LABEL 3 0093-5234 TABLET, FILM COATED 600 mg ORAL ANDA 30 sections
Efavirenz HUMAN PRESCRIPTION DRUG LABEL 1 0378-2233 TABLET, FILM COATED 600 mg ORAL ANDA 26 sections
Atripla HUMAN PRESCRIPTION DRUG LABEL 3 15584-0101 TABLET, FILM COATED 600 mg ORAL NDA 34 sections
Efavirenz Human Prescription Drug Label 1 31722-504 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
Efavirenz, Emtricitabine and Tenofovir Disoproxil Fumarate Human Prescription Drug Label 3 33342-138 TABLET, FILM COATED 600 mg ORAL ANDA 30 sections
Efavirenz, emtricitabine and tenofovir disoproxil fumarate Human Prescription Drug Label 3 42385-915 TABLET, FILM COATED 600 mg ORAL ANDA 30 sections
Efavirenz, Lamivudine and Tenofovir Disoproxil Fumarate Human Prescription Drug Label 3 42385-928 TABLET, FILM COATED 600 mg ORAL ANDA 30 sections
Efavirenz, Lamivudine and Tenofovir Disoproxil Fumarate Human Prescription Drug Label 3 42385-929 TABLET, FILM COATED 400 mg ORAL ANDA 30 sections
Efavirenz HUMAN PRESCRIPTION DRUG LABEL 1 42543-889 TABLET 600 mg ORAL ANDA 26 sections
SYMFI LO HUMAN PRESCRIPTION DRUG LABEL 3 49502-425 TABLET, FILM COATED 400 mg ORAL NDA 32 sections
SYMFI HUMAN PRESCRIPTION DRUG LABEL 3 49502-475 TABLET, FILM COATED 600 mg ORAL NDA 31 sections
Efavirenz HUMAN PRESCRIPTION DRUG LABEL 1 51407-382 TABLET 600 mg ORAL ANDA 26 sections
Atripla HUMAN PRESCRIPTION DRUG LABEL 3 53808-0208 TABLET, FILM COATED 600 mg ORAL NDA 31 sections
SUSTIVA HUMAN PRESCRIPTION DRUG LABEL 1 54868-4668 TABLET, FILM COATED 600 mg ORAL NDA 29 sections
Atripla HUMAN PRESCRIPTION DRUG LABEL 3 54868-5643 TABLET, FILM COATED 600 mg ORAL NDA 31 sections
Atripla Access HUMAN PRESCRIPTION DRUG LABEL 3 61958-1601 TABLET, FILM COATED 600 mg ORAL EXPORT ONLY 34 sections
Efavirenz HUMAN PRESCRIPTION DRUG LABEL 1 64380-889 TABLET 600 mg ORAL ANDA 18 sections
Efavirenz Human Prescription Drug Label 1 64980-406 CAPSULE 50 mg ORAL ANDA 29 sections
Efavirenz Human Prescription Drug Label 1 64980-407 CAPSULE 200 mg ORAL ANDA 29 sections
Efavirenz Human Prescription Drug Label 1 65862-049 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
Efavirenz Human Prescription Drug Label 1 65862-104 CAPSULE 50 mg ORAL ANDA 29 sections
Efavirenz Human Prescription Drug Label 1 65862-104 CAPSULE 50 mg ORAL ANDA 29 sections
Efavirenz Human Prescription Drug Label 1 65862-105 CAPSULE 100 mg ORAL ANDA 29 sections
Efavirenz Human Prescription Drug Label 1 65862-105 CAPSULE 100 mg ORAL ANDA 29 sections
Efavirenz Human Prescription Drug Label 1 65862-106 CAPSULE 200 mg ORAL ANDA 29 sections
Efavirenz Human Prescription Drug Label 1 65862-106 CAPSULE 200 mg ORAL ANDA 29 sections
Efavirenz, Emtricitabine And Tenofovir Disoproxil Fumarate Human Prescription Drug Label 3 65862-497 TABLET, FILM COATED 600 mg ORAL ANDA 30 sections