efavirenz 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 42.50 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
fu (Fraction unbound in plasma) 0.01 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.478 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.726 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 40.087 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 15.488 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 0.450 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 1.360 % High 1
herg hERG pIC50 4.973 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 7.852 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 9.840 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.350 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MAPK7,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,TEK 20
kinase-selectivity-class AXL,PDK1,PDK2 3
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 3.034 High 1
mh-clint Mouse hepatocyte intrinsic clearance 51.761 High 1
mppb Mouse plasma protein binding (% unbound) 0.610 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 4.446 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 1
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 0.430 % High 1
rh-clint Rat hepatocyte intrinsic clearance 37.670 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 5.570 % High 1
rppb Rat plasma protein binding (% unbound) 0.310 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 2.992 uM High 1

Approvals:

DateAgencyCompanyOrphan
Sept. 17, 1998 FDA BRISTOL MYERS SQUIBB
May 28, 1999 EMA Bristol-Myers Squibb Pharma EEIG

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
Viral mutation identified 726.16 31.53 130 7974 1895 90618448
Virologic failure 617.42 31.53 115 7989 2109 90618234
Abortion spontaneous 593.27 31.53 211 7893 53845 90566498
Maternal exposure during pregnancy 577.75 31.53 372 7732 359691 90260652
Immune reconstitution inflammatory syndrome 464.84 31.53 111 7993 6908 90613435
Abortion induced 365.21 31.53 102 8002 11786 90608557
Pathogen resistance 349.90 31.53 91 8013 8024 90612319
Stillbirth 347.87 31.53 89 8015 7354 90612989
Drug resistance 345.50 31.53 122 7982 30327 90590016
Pregnancy 267.66 31.53 124 7980 61923 90558420
Foetal exposure during pregnancy 250.12 31.53 106 7998 42869 90577474
Exposure during pregnancy 246.50 31.53 189 7915 238221 90382122
Normal newborn 199.57 31.53 76 8028 23286 90597057
Lipodystrophy acquired 182.09 31.53 39 8065 1475 90618868
Blood HIV RNA increased 174.71 31.53 34 8070 790 90619553
Caesarean section 160.68 31.53 61 8043 18516 90601827
Treatment noncompliance 150.16 31.53 79 8025 51648 90568695
Premature delivery 111.89 31.53 59 8045 38703 90581640
Cerebellar ataxia 106.63 31.53 23 8081 899 90619444
Viral load increased 104.96 31.53 25 8079 1531 90618812
Birth mark 101.59 31.53 17 8087 161 90620182
Pregnancy with implant contraceptive 96.20 31.53 28 8076 3733 90616610
Paroxysmal extreme pain disorder 92.93 31.53 15 8089 111 90620232
Congenital umbilical hernia 90.80 31.53 17 8087 319 90620024
Pulmonary tuberculosis 89.27 31.53 28 8076 4806 90615537
Pregnancy on contraceptive 88.35 31.53 21 8083 1274 90619069
Degenerative bone disease 86.95 31.53 16 8088 272 90620071
Chronic respiratory disease 86.25 31.53 16 8088 285 90620058
Confusional arousal 85.83 31.53 16 8088 293 90620050
Live birth 84.23 31.53 64 8040 79043 90541300
Post procedural hypothyroidism 82.40 31.53 16 8088 367 90619976
Neurotoxicity 80.45 31.53 39 8065 21428 90598915
Lactic acidosis 77.32 31.53 51 8053 50412 90569931
Drug interaction 74.92 31.53 107 7997 276346 90343997
Fanconi syndrome acquired 73.26 31.53 18 8086 1256 90619087
Immune reconstitution inflammatory syndrome associated tuberculosis 72.20 31.53 15 8089 488 90619855
Autoimmune hepatitis 71.87 31.53 29 8075 10322 90610021
Portal hypertension 69.50 31.53 23 8081 4678 90615665
Dyslipidaemia 65.67 31.53 27 8077 10080 90610263
Mouth injury 64.41 31.53 16 8088 1168 90619175
Cleft lip and palate 60.74 31.53 14 8090 742 90619601
Anaemia 53.14 31.53 105 7999 352697 90267646
Tongue discomfort 50.98 31.53 16 8088 2749 90617594
Tuberculosis 50.66 31.53 24 8080 12525 90607818
Meningitis cryptococcal 48.44 31.53 14 8090 1819 90618524
Malaria 46.45 31.53 9 8095 204 90620139
Cholestatic liver injury 46.00 31.53 16 8088 3781 90616562
Ultrasound antenatal screen 45.92 31.53 9 8095 217 90620126
Fatigue 44.58 31.53 24 8080 1153999 89466344
Nephropathy toxic 44.39 31.53 22 8082 12666 90607677
Premature rupture of membranes 43.56 31.53 17 8087 5541 90614802
Hydrops foetalis 42.13 31.53 10 8094 603 90619740
Gene mutation 42.10 31.53 13 8091 2117 90618226
Polymyalgia rheumatica 41.78 31.53 16 8088 4961 90615382
Spinocerebellar disorder 41.62 31.53 6 8098 18 90620325
Peptic ulcer 40.29 31.53 16 8088 5459 90614884
Encephalopathy 39.60 31.53 33 8071 46411 90573932
Rash maculo-papular 38.94 31.53 31 8073 40902 90579441
Abnormal dreams 37.85 31.53 19 8085 11238 90609105
CD4 lymphocytes decreased 37.28 31.53 11 8093 1536 90618807
Ectopic pregnancy 36.75 31.53 13 8091 3228 90617115
Pregnancy on oral contraceptive 36.19 31.53 10 8094 1105 90619238
Endometrial sarcoma 35.50 31.53 5 8099 12 90620331
Twin pregnancy 35.11 31.53 10 8094 1233 90619110
Bundle branch block left 34.67 31.53 16 8088 7869 90612474
Neural tube defect 34.54 31.53 7 8097 201 90620142
Encephalocele 34.47 31.53 7 8097 203 90620140
Foetal death 34.31 31.53 22 8082 20701 90599642
Retinal toxicity 33.78 31.53 10 8094 1412 90618931
Alanine aminotransferase increased 33.74 31.53 47 8057 118291 90502052
Viral load abnormal 33.29 31.53 4 8100 0 90620343
Pachygyria 33.29 31.53 4 8100 0 90620343
Premature baby 32.81 31.53 23 8081 25054 90595289
Aspartate aminotransferase increased 32.56 31.53 43 8061 102894 90517449
Hepatomegaly 32.08 31.53 18 8086 13308 90607035
Gingivitis 32.05 31.53 16 8088 9353 90610990
Unintended pregnancy 32.04 31.53 15 8089 7622 90612721

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 1548.38 19.31 785 15817 110578 42494155
Drug interaction 1252.68 19.31 939 15663 266060 42338673
Immune reconstitution inflammatory syndrome 889.44 19.31 273 16329 9870 42594863
Viral mutation identified 830.31 19.31 204 16398 3127 42601606
Virologic failure 822.95 19.31 210 16392 3784 42600949
Pathogen resistance 639.62 19.31 219 16383 11231 42593502
Lipodystrophy acquired 597.28 19.31 158 16444 3292 42601441
Psychiatric decompensation 533.81 19.31 151 16451 4071 42600662
Depression suicidal 474.09 19.31 130 16472 3115 42601618
Tearfulness 468.92 19.31 131 16471 3369 42601364
Depressive symptom 412.09 19.31 121 16481 3732 42601001
Psychomotor skills impaired 376.25 19.31 121 16481 5083 42599650
Loss of personal independence in daily activities 349.53 19.31 226 16376 49590 42555143
Mitochondrial toxicity 319.07 19.31 91 16511 2524 42602209
Paranoia 297.53 19.31 133 16469 13893 42590840
Progressive external ophthalmoplegia 279.72 19.31 72 16530 1339 42603394
Eyelid ptosis 257.13 19.31 97 16505 6564 42598169
Drug resistance 256.49 19.31 162 16440 34086 42570647
Psychotic disorder 233.41 19.31 144 16458 29064 42575669
Suicidal ideation 170.77 19.31 145 16457 48016 42556717
Foetal exposure during pregnancy 152.67 19.31 135 16467 47176 42557557
Treatment failure 129.42 19.31 140 16462 62484 42542249
Diplopia 124.89 19.31 85 16517 20231 42584502
Pulmonary tuberculosis 103.44 19.31 48 16554 5453 42599280
Psychomotor retardation 100.58 19.31 44 16558 4355 42600378
Retinal toxicity 100.10 19.31 26 16576 501 42604232
Lipoatrophy 99.48 19.31 25 16577 420 42604313
Multiple-drug resistance 87.61 19.31 47 16555 7275 42597458
Trisomy 18 87.35 19.31 26 16576 839 42603894
Hydrops foetalis 86.19 19.31 26 16576 879 42603854
Cleft lip and palate 85.44 19.31 26 16576 906 42603827
Prescribed overdose 81.61 19.31 55 16547 12872 42591861
CD4 lymphocytes decreased 81.51 19.31 30 16572 1891 42602842
Ophthalmoplegia 81.12 19.31 31 16571 2169 42602564
Treatment noncompliance 77.38 19.31 84 16518 37588 42567145
Anxiety 75.60 19.31 152 16450 118408 42486325
Blood HIV RNA increased 75.55 19.31 27 16575 1564 42603169
Ultrasound antenatal screen 70.46 19.31 20 16582 544 42604189
Hepatic fibrosis 66.04 19.31 34 16568 4838 42599895
Off label use 63.94 19.31 94 16508 638241 41966492
Abnormal dreams 61.51 19.31 39 16563 8232 42596501
HIV-associated neurocognitive disorder 60.48 19.31 16 16586 332 42604401
Hyperlipidaemia 58.82 19.31 56 16546 21460 42583273
Fanconi syndrome acquired 58.26 19.31 24 16578 2046 42602687
Dyslipidaemia 56.89 19.31 39 16563 9379 42595354
Gynaecomastia 55.38 19.31 43 16559 12524 42592209
Fanconi syndrome 54.60 19.31 22 16580 1772 42602961
Meningitis cryptococcal 53.61 19.31 26 16576 3257 42601476
Portal hypertension 49.74 19.31 28 16574 4759 42599974
Abortion spontaneous 49.00 19.31 14 16588 390 42604343
Pneumonia 47.40 19.31 57 16545 422092 42182641
Drug ineffective 45.35 19.31 113 16489 630084 41974649
Pain 44.30 19.31 20 16582 244828 42359905
Immune reconstitution inflammatory syndrome associated tuberculosis 43.98 19.31 14 16588 567 42604166
Hypertriglyceridaemia 43.21 19.31 34 16568 10092 42594641
Osteoporosis 43.04 19.31 40 16562 14866 42589867
Dyspnoea 41.48 19.31 68 16534 442553 42162180
Retroviral rebound syndrome 41.35 19.31 7 16595 11 42604722
Lymph node tuberculosis 41.14 19.31 13 16589 514 42604219
Hydrocele 40.81 19.31 20 16582 2563 42602170
Fatigue 40.75 19.31 67 16535 435574 42169159
Hyperlactacidaemia 40.49 19.31 24 16578 4492 42600241
Secondary syphilis 39.94 19.31 9 16593 92 42604641
Life expectancy shortened 39.85 19.31 8 16594 44 42604689
Renal impairment 39.43 19.31 113 16489 110115 42494618
Atrial fibrillation 37.52 19.31 5 16597 139588 42465145
Tuberculoid leprosy 37.37 19.31 8 16594 63 42604670
Fall 36.77 19.31 23 16579 234497 42370236
Constipation 36.76 19.31 9 16593 162282 42442451
Urinary tract inflammation 36.50 19.31 10 16592 238 42604495
Neuropsychiatric symptoms 36.27 19.31 13 16589 759 42603974
Kaposi's sarcoma 35.90 19.31 13 16589 782 42603951
Nephropathy toxic 35.35 19.31 38 16564 16800 42587933
Viral load increased 35.18 19.31 19 16583 2978 42601755
Hepatitis C 34.81 19.31 30 16572 10103 42594630
Nervous system disorder 34.69 19.31 38 16564 17157 42587576
Product dose omission issue 34.11 19.31 9 16593 154356 42450377
Conductive deafness 33.21 19.31 11 16591 506 42604227
Hypotension 33.08 19.31 31 16571 257600 42347133
Congenital umbilical hernia 32.92 19.31 10 16592 346 42604387
Tuberculosis 32.89 19.31 29 16573 10070 42594663
Hepatosplenomegaly 32.24 19.31 21 16581 4639 42600094
Back pain 31.84 19.31 8 16594 141768 42462965
Malignant neoplasm progression 31.34 19.31 3 16599 108397 42496336
Developmental hip dysplasia 29.08 19.31 9 16593 332 42604401
Death 28.96 19.31 91 16511 471094 42133639
Intentional product use issue 27.99 19.31 76 16526 71757 42532976
Intracranial pressure increased 27.39 19.31 19 16583 4655 42600078
Night blindness 26.97 19.31 8 16594 255 42604478
Meningitis tuberculous 26.59 19.31 10 16592 669 42604064
Blood pressure increased 26.56 19.31 4 16598 101924 42502809
Renal tubular disorder 26.55 19.31 19 16583 4890 42599843
Renal tubular dysfunction 26.55 19.31 9 16593 445 42604288
Proteinuria 25.91 19.31 38 16564 22945 42581788
Birth mark 25.65 19.31 7 16595 164 42604569
Drug-induced liver injury 25.45 19.31 50 16552 38223 42566510
Febrile neutropenia 25.44 19.31 21 16581 185682 42419051
COVID-19 25.16 19.31 7 16595 115941 42488792
Sickle cell disease 25.14 19.31 7 16595 177 42604556
Blood triglycerides increased 25.14 19.31 31 16571 15865 42588868
Paradoxical drug reaction 24.85 19.31 18 16584 4720 42600013
Cystitis noninfective 24.79 19.31 9 16593 545 42604188
Aspartate aminotransferase increased 24.62 19.31 76 16526 77087 42527646
Mitochondrial myopathy 24.40 19.31 7 16595 198 42604535
Histoplasmosis disseminated 23.83 19.31 13 16589 2078 42602655
Toxoplasma serology positive 23.74 19.31 4 16598 6 42604727
Alanine aminotransferase increased 23.65 19.31 82 16520 88324 42516409
Cryptococcosis 23.52 19.31 15 16587 3196 42601537
Drug abuse 23.34 19.31 6 16596 104765 42499968
Pain in extremity 23.27 19.31 15 16587 150589 42454144
Cytomegalovirus chorioretinitis 23.01 19.31 17 16585 4594 42600139
Incorrect route of product administration 22.92 19.31 37 16565 24268 42580465
Polyneuropathy chronic 22.11 19.31 5 16597 52 42604681
Mycobacterium avium complex infection 21.82 19.31 14 16588 3013 42601720
Acquired immunodeficiency syndrome 21.80 19.31 8 16594 500 42604233
Hepatic function abnormal 21.54 19.31 56 16546 51511 42553222
Hepatic cirrhosis 21.38 19.31 32 16570 19670 42585063
Hepatitis B 21.31 19.31 19 16583 6692 42598041
Pulmonary hilar enlargement 21.18 19.31 4 16598 15 42604718
Lipids increased 21.01 19.31 10 16592 1202 42603531
Limb deformity 20.78 19.31 8 16594 571 42604162
Osteomalacia 20.72 19.31 9 16593 875 42603858
Liver injury 20.64 19.31 31 16571 19117 42585616
Nasopharyngitis 20.34 19.31 4 16598 83992 42520741
Elbow synostosis 20.25 19.31 4 16598 20 42604713
Blood lactic acid increased 20.23 19.31 20 16582 8019 42596714
Cachexia 20.09 19.31 20 16582 8084 42596649
Glycosuria 19.84 19.31 10 16592 1360 42603373
Hepatitis 19.79 19.31 37 16565 27263 42577470
Congenital tuberculosis 19.63 19.31 4 16598 24 42604709
Vanishing bile duct syndrome 19.59 19.31 11 16591 1860 42602873
Eyelid ptosis congenital 19.47 19.31 5 16597 92 42604641

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 1414.05 20.64 367 19492 15859 110553581
Drug interaction 970.81 20.64 763 19096 499420 110070020
Viral mutation identified 929.91 20.64 204 19655 4215 110565225
Virologic failure 906.77 20.64 204 19655 4748 110564692
Depression 881.75 20.64 602 19257 316733 110252707
Lipodystrophy acquired 766.78 20.64 175 19684 4349 110565091
Drug resistance 631.70 20.64 271 19588 56103 110513337
Psychiatric decompensation 598.00 20.64 150 19709 5615 110563825
Pathogen resistance 550.83 20.64 180 19679 17492 110551948
Depression suicidal 527.75 20.64 131 19728 4693 110564747
Tearfulness 486.08 20.64 134 19725 7261 110562179
Psychomotor skills impaired 427.68 20.64 120 19739 6938 110562502
Depressive symptom 411.22 20.64 121 19738 8293 110561147
Mitochondrial toxicity 399.95 20.64 97 19762 3148 110566292
Abortion spontaneous 364.73 20.64 159 19700 34123 110535317
Paranoia 343.91 20.64 135 19724 22239 110547201
Progressive external ophthalmoplegia 334.69 20.64 72 19787 1348 110568092
Loss of personal independence in daily activities 282.63 20.64 226 19633 149794 110419646
Psychotic disorder 270.85 20.64 147 19712 50790 110518650
Abortion induced 259.17 20.64 84 19775 7935 110561505
Eyelid ptosis 253.65 20.64 94 19765 13233 110556207
Blood HIV RNA increased 217.25 20.64 55 19804 2133 110567307
Stillbirth 215.70 20.64 63 19796 4201 110565239
Pulmonary tuberculosis 205.81 20.64 73 19786 9066 110560374
Maternal exposure during pregnancy 189.58 20.64 231 19628 254652 110314788
Suicidal ideation 184.22 20.64 145 19714 93792 110475648
Caesarean section 146.59 20.64 64 19795 13753 110555687
Treatment noncompliance 145.95 20.64 114 19745 72876 110496564
Portal hypertension 142.89 20.64 55 19804 8582 110560858
Retinal toxicity 141.74 20.64 37 19822 1622 110567818
CD4 lymphocytes decreased 133.22 20.64 40 19819 2934 110566506
Fanconi syndrome acquired 128.15 20.64 39 19820 2995 110566445
Hydrops foetalis 125.78 20.64 29 19830 752 110568688
Diplopia 123.94 20.64 83 19776 41811 110527629
Ultrasound antenatal screen 117.90 20.64 27 19832 679 110568761
Exposure during pregnancy 116.71 20.64 147 19712 167277 110402163
Lipoatrophy 115.34 20.64 26 19833 608 110568832
Pregnancy 111.36 20.64 84 19775 50983 110518457
HIV-associated neurocognitive disorder 109.32 20.64 23 19836 385 110569055
Cleft lip and palate 106.35 20.64 25 19834 707 110568733
Trisomy 18 105.05 20.64 24 19835 597 110568843
Multiple-drug resistance 104.75 20.64 50 19809 13185 110556255
Immune reconstitution inflammatory syndrome associated tuberculosis 102.20 20.64 26 19833 1028 110568412
Pain 100.84 20.64 24 19835 954931 109614509
Meningitis cryptococcal 99.53 20.64 36 19823 4726 110564714
Viral load increased 99.40 20.64 33 19826 3357 110566083
Psychomotor retardation 98.92 20.64 41 19818 7751 110561689
Nephropathy toxic 92.41 20.64 59 19800 27419 110542021
Ophthalmoplegia 86.20 20.64 30 19829 3520 110565920
Gynaecomastia 84.83 20.64 39 19820 9451 110559989
Lactic acidosis 83.70 20.64 93 19766 92718 110476722
Tuberculosis 79.97 20.64 46 19813 17728 110551712
Pregnancy on contraceptive 79.02 20.64 21 19838 987 110568453
Dyslipidaemia 73.65 20.64 42 19817 15923 110553517
Hepatic fibrosis 71.63 20.64 33 19826 8033 110561407
Fanconi syndrome 67.59 20.64 25 19834 3494 110565946
Lymph node tuberculosis 63.36 20.64 18 19841 1086 110568354
Joint swelling 58.15 20.64 6 19853 442839 110126601
Aspartate aminotransferase increased 56.13 20.64 102 19757 159834 110409606
Fatigue 54.57 20.64 84 19775 1215874 109353566
Pregnancy with implant contraceptive 53.59 20.64 19 19840 2353 110567087
Hyperlipidaemia 52.92 20.64 47 19812 35801 110533639
Anxiety 52.09 20.64 158 19701 344920 110224520
Cytomegalovirus chorioretinitis 50.59 20.64 25 19834 7103 110562337
Hypertriglyceridaemia 50.16 20.64 33 19826 16121 110553319
Normal newborn 49.91 20.64 37 19822 21859 110547581
Renal tubular dysfunction 48.78 20.64 14 19845 876 110568564
Alanine aminotransferase increased 48.51 20.64 104 19755 183669 110385771
Hepatomegaly 48.39 20.64 36 19823 21378 110548062
Dyspnoea 48.17 20.64 78 19781 1106794 109462646
Meningitis tuberculous 47.93 20.64 15 19844 1263 110568177
Autoimmune hepatitis 47.82 20.64 31 19828 14773 110554667
Foetal exposure during pregnancy 46.47 20.64 24 19835 7481 110561959
Secondary syphilis 46.20 20.64 9 19850 100 110569340
Tuberculoid leprosy 45.56 20.64 9 19850 108 110569332
Arthralgia 45.31 20.64 44 19815 779588 109789852
Osteomalacia 44.74 20.64 15 19844 1572 110567868
Cholestatic liver injury 43.99 20.64 23 19836 7353 110562087
Mycobacterium avium complex infection 42.87 20.64 21 19838 5856 110563584
Infection 42.52 20.64 7 19852 362193 110207247
Rheumatoid arthritis 42.21 20.64 3 19856 299610 110269830
Abnormal dreams 41.87 20.64 27 19832 12753 110556687
Cachexia 41.44 20.64 27 19832 12978 110556462
Night blindness 39.83 20.64 11 19848 598 110568842
Tuberculoma of central nervous system 39.69 20.64 11 19848 606 110568834
Urinary tract inflammation 39.48 20.64 10 19849 388 110569052
Premature delivery 39.05 20.64 37 19822 30595 110538845
Hyperlactacidaemia 38.76 20.64 22 19837 8264 110561176
Cryptococcosis 38.19 20.64 18 19841 4613 110564827
Anaemia 37.86 20.64 196 19663 546890 110022550
Abdominal discomfort 37.53 20.64 12 19847 393846 110175594
Hepatitis C 37.38 20.64 25 19834 12548 110556892
Conductive deafness 36.89 20.64 9 19850 299 110569141
Lymphadenopathy 36.63 20.64 51 19808 63784 110505656
Swelling 36.59 20.64 9 19850 351032 110218408
Fall 36.28 20.64 33 19826 603449 109965991
Prescribed overdose 36.11 20.64 60 19799 87521 110481919
Hepatitis B 35.73 20.64 22 19837 9590 110559850
Acquired immunodeficiency syndrome 35.54 20.64 9 19850 349 110569091
Pain in extremity 35.22 20.64 22 19837 487096 110082344
Pneumonia 35.15 20.64 65 19794 876649 109692791
Alopecia 34.95 20.64 11 19848 364742 110204698
Off label use 34.35 20.64 146 19713 1500039 109069401
Endometrial sarcoma 34.19 20.64 5 19854 6 110569434
Neurotoxicity 34.14 20.64 40 19819 42167 110527273
Hepatosplenomegaly 34.07 20.64 19 19840 6900 110562540
Renal impairment 33.94 20.64 92 19767 188353 110381087
Intracranial pressure increased 33.88 20.64 22 19837 10513 110558927
Pneumocystis jirovecii pneumonia 33.74 20.64 40 19819 42695 110526745
Gene mutation 33.52 20.64 15 19844 3414 110566026
Disseminated tuberculosis 33.44 20.64 17 19842 5129 110564311
Therapeutic product effect decreased 32.87 20.64 3 19856 244313 110325127
Blood triglycerides increased 32.62 20.64 30 19829 23896 110545544
Oral candidiasis 32.25 20.64 40 19819 44720 110524720
Product dose omission issue 32.11 20.64 9 19850 321773 110247667
Retroviral rebound syndrome 32.01 20.64 5 19854 12 110569428
Systemic lupus erythematosus 31.98 20.64 4 19855 254334 110315106
Drug-induced liver injury 31.72 20.64 68 19791 119999 110449441
Neuropsychiatric symptoms 31.72 20.64 11 19848 1277 110568163
Extrapulmonary tuberculosis 31.54 20.64 9 19850 552 110568888
Pregnancy on oral contraceptive 31.11 20.64 10 19849 918 110568522
Proteinuria 30.84 20.64 37 19822 39981 110529459
Drug ineffective 30.64 20.64 155 19704 1520385 109049055
Renal tubular disorder 30.18 20.64 18 19841 7411 110562029
Kaposi's sarcoma 29.54 20.64 9 19850 693 110568747
Musculoskeletal stiffness 29.50 20.64 7 19852 279815 110289625
Back pain 29.32 20.64 15 19844 370981 110198459
Constipation 28.98 20.64 14 19845 357772 110211668
Nightmare 28.44 20.64 35 19824 38828 110530612
HIV infection CDC category C 27.99 20.64 5 19854 33 110569407
Paradoxical drug reaction 27.94 20.64 19 19840 9798 110559642
Atrial fibrillation 27.94 20.64 4 19855 229638 110339802
Wheezing 27.67 20.64 6 19853 255224 110314216
Intentional product use issue 27.17 20.64 102 19757 247804 110321636
Hepatotoxicity 26.90 20.64 44 19815 63356 110506084
Premature rupture of membranes 26.35 20.64 14 19845 4623 110564817
Febrile neutropenia 26.26 20.64 12 19847 316755 110252685
Type III hyperlipidaemia 26.11 20.64 4 19855 8 110569432
Hypophosphataemia 26.10 20.64 31 19828 33151 110536289
Inappropriate schedule of product administration 26.10 20.64 3 19856 203634 110365806
Aplasia pure red cell 25.99 20.64 18 19841 9560 110559880
CD4 lymphocytes 25.79 20.64 4 19855 9 110569431
Hepatic function abnormal 25.24 20.64 52 19807 89243 110480197
Urticaria 25.03 20.64 13 19846 318844 110250596
Asthma 24.97 20.64 7 19852 250284 110319156
Cushingoid 24.93 20.64 19 19840 11693 110557747
Abdominal pain upper 24.90 20.64 16 19843 349095 110220345
Central nervous system immune reconstitution inflammatory response 24.80 20.64 5 19854 67 110569373
Therapeutic product effect incomplete 24.80 20.64 5 19854 223800 110345640
Malaria 24.68 20.64 7 19852 420 110569020
Stomatitis 24.40 20.64 9 19850 270233 110299207
Mitochondrial myopathy 24.25 20.64 7 19852 447 110568993
Progressive multifocal leukoencephalopathy 24.21 20.64 26 19833 24930 110544510
Glycosuria 24.10 20.64 11 19848 2619 110566821
Folate deficiency 24.10 20.64 13 19846 4425 110565015
Acute myocardial infarction 23.93 20.64 49 19810 83728 110485712
Nervous system disorder 23.91 20.64 29 19830 31692 110537748
Osteoporosis 23.76 20.64 50 19809 87102 110482338
Jaundice 23.64 20.64 40 19819 59196 110510244
Genotype drug resistance test positive 23.42 20.64 9 19850 1397 110568043
Discomfort 23.37 20.64 5 19854 214702 110354738
Blister 23.36 20.64 6 19853 227370 110342070
Dry mouth 23.15 20.64 4 19855 199944 110369496
Mobility decreased 23.02 20.64 7 19852 237415 110332025
Meningomyelocele 23.02 20.64 4 19855 22 110569418
Visual field defect 22.91 20.64 17 19842 10055 110559385
Twin pregnancy 22.89 20.64 8 19851 950 110568490
Osteoarthritis 22.64 20.64 3 19856 182620 110386820
Malaise 22.55 20.64 55 19804 671764 109897676
Drug intolerance 22.36 20.64 24 19835 406488 110162952
Ectopic pregnancy 22.30 20.64 10 19849 2287 110567153
Hepatic cirrhosis 22.28 20.64 42 19817 67584 110501856
Cerebral toxoplasmosis 22.24 20.64 11 19848 3131 110566309
Vanishing bile duct syndrome 22.15 20.64 11 19848 3157 110566283
Skin lesion 22.13 20.64 36 19823 51595 110517845
Nodular regenerative hyperplasia 22.12 20.64 9 19850 1622 110567818
Skin atrophy 21.83 20.64 14 19845 6550 110562890
Hepatic cytolysis 21.74 20.64 37 19822 55016 110514424
Hyperphosphaturia 21.45 20.64 5 19854 136 110569304
Lipids abnormal 21.41 20.64 7 19852 678 110568762
Malignant neoplasm progression 21.33 20.64 3 19856 174564 110394876
CSF HIV escape syndrome 21.30 20.64 6 19853 351 110569089
HIV associated nephropathy 21.22 20.64 6 19853 356 110569084
Rash scarlatiniform 21.12 20.64 6 19853 362 110569078
Blood pressure increased 21.08 20.64 10 19849 258363 110311077
CD4 lymphocytes increased 20.99 20.64 6 19853 370 110569070
Oesophageal candidiasis 20.86 20.64 17 19842 11517 110557923
COVID-19 20.75 20.64 9 19850 245051 110324389
Renal tubular acidosis 20.67 20.64 12 19847 4703 110564737

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 D004791 Enzyme Inhibitors
MeSH PA D018894 Reverse Transcriptase Inhibitors
MeSH PA D019384 Nucleic Acid Synthesis Inhibitors
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D065688 Cytochrome P-450 CYP2C9 Inhibitors
MeSH PA D065689 Cytochrome P-450 CYP2C19 Inhibitors
MeSH PA D065695 Cytochrome P-450 CYP2B6 Inducers
MeSH PA D065701 Cytochrome P-450 CYP3A Inducers
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:22587 antiviral agent
CHEBI has role CHEBI:33231 antitubercular agent
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:36044 antiviral drug
CHEBI has role CHEBI:38068 antimalarial
CHEBI has role CHEBI:53756 HIV-1 reverse transcriptase inhibitor
CHEBI has role CHEBI:64946 anti-HIV agent

Related Drugs by ATC class:

J05AG Non-nucleoside reverse transcriptase inhibitors 5 drugs
delavirdinedoravirineetravirinenevirapinerilpivirine
J05AR Antivirals for treatment of HIV infections, combinations 19 drugs
abacaviratazanavirbictegravircobicistatdarunavirdolutegravirdoravirineelvitegraviremtricitabinelamivudinelopinavirnevirapine 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
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
Hypokalemia contraindication 43339004
Cardiovascular disease contraindication 49601007 DOID:1287
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
Prolonged QT interval contraindication 111975006
Chronic hepatitis C contraindication 128302006
Seizure disorder contraindication 128613002
Liver function tests abnormal contraindication 166603001
Hypomagnesemia contraindication 190855004
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
Family history of sudden death contraindication 430283008




🐶 Veterinary Drug Use

None

🐶 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 **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 DISCN TABLET ORAL 9018192 June 13, 2026 TREATMENT OF HIV-1 INFECTION IN ADULTS
600MG;200MG;300MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 DISCN TABLET ORAL 9018192 June 13, 2026 TREATMENT OF HIV-1 INFECTION IN PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER
600MG;200MG;300MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 DISCN TABLET ORAL 9545414 June 13, 2026 TREATMENT OF HIV-1 INFECTION IN ADULTS
600MG;200MG;300MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** ATRIPLA GILEAD SCIENCES N021937 July 12, 2006 DISCN 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
ATP-binding cassette sub-family G member 2 Transporter IC50 4.69 CHEMBL
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 Enzyme Ki 8.07 CHEMBL
Envelope glycoprotein gp160 [Cleaved into: Surface protein gp120 Viral envelope protein 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
JE6H2O27P8 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Efavirenz, Emtricitabine and Tenofovir Disoproxil Fumarate HUMAN PRESCRIPTION DRUG LABEL 3 0093-5234 TABLET, FILM COATED 600 mg ORAL ANDA 29 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 31722-736 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
Efavirenz Human Prescription Drug Label 1 33342-013 TABLET 600 mg ORAL ANDA 26 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
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
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
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 28 sections
Efavirenz Human Prescription Drug Label 1 65862-105 CAPSULE 100 mg ORAL ANDA 28 sections
Efavirenz Human Prescription Drug Label 1 65862-106 CAPSULE 200 mg ORAL ANDA 28 sections
Efavirenz, Emtricitabine And Tenofovir Disoproxil Fumarate Human Prescription Drug Label 3 65862-497 TABLET, FILM COATED 600 mg ORAL ANDA 29 sections
efavirenz, emtricitabine and tenofovir disoproxil fumarate HUMAN PRESCRIPTION DRUG LABEL 3 69097-210 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
Efavirenz HUMAN PRESCRIPTION DRUG LABEL 1 69097-301 TABLET, FILM COATED 600 mg ORAL ANDA 25 sections
Efavirenz, Emtricitabine And Tenofovir Disoproxil Fumarate HUMAN PRESCRIPTION DRUG LABEL 3 72162-2565 TABLET, FILM COATED 600 mg ORAL ANDA 29 sections
EFAVIRENZ HUMAN PRESCRIPTION DRUG LABEL 1 72865-172 TABLET, FILM COATED 600 mg ORAL ANDA 29 sections
efavirenz, emtricitabine and tenofovir disoproxil fumarate HUMAN PRESCRIPTION DRUG LABEL 3 76282-678 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections