atazanavir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
HIV protease inhibitors 254 198904-31-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • BMS-232632
  • atazanavir
  • reyataz
  • atazanavir sulphate
  • atazanavir sulfate
An azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS. There was some evidence of in vitro activity against SARS-CoV-2, but no clinical trial data was found to support use in the treatment of COVID-19.
  • Molecular weight: 704.87
  • Formula: C38H52N6O7
  • CLOGP: 5.92
  • LIPINSKI: 3
  • HAC: 13
  • HDO: 5
  • TPSA: 171.22
  • ALOGS: -5.33
  • ROTB: 18
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.30 g O
0.30 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 7 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 8.11 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 64 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
March 2, 2004 EMA
June 20, 2003 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 1009.08 27.21 339 8543 46856 63433284
Foetal exposure during pregnancy 950.11 27.21 295 8587 31667 63448473
Maternal exposure during pregnancy 743.72 27.21 430 8452 219632 63260508
Exposure during pregnancy 500.04 27.21 295 8587 155252 63324888
Abortion induced 426.93 27.21 123 8759 10119 63470021
Premature baby 356.73 27.21 127 8755 20608 63459532
Live birth 309.15 27.21 121 8761 25509 63454631
Stillbirth 294.34 27.21 84 8798 6666 63473474
Caesarean section 258.00 27.21 95 8787 16937 63463203
Pregnancy 254.20 27.21 117 8765 36719 63443421
Hyperbilirubinaemia 251.58 27.21 84 8798 11230 63468910
Premature delivery 240.12 27.21 106 8776 30175 63449965
Drug interaction 178.01 27.21 188 8694 228943 63251197
Foetal death 150.70 27.21 57 8825 10923 63469217
Virologic failure 146.71 27.21 37 8845 1825 63478315
Foetal growth restriction 128.75 27.21 46 8836 7507 63472633
Pregnancy on contraceptive 120.81 27.21 29 8853 1163 63478977
Normal newborn 116.98 27.21 44 8838 8297 63471843
Viral mutation identified 113.54 27.21 30 8852 1780 63478360
Congenital naevus 112.73 27.21 20 8862 168 63479972
Ventricular septal defect 107.28 27.21 35 8847 4343 63475797
Jaundice 105.39 27.21 60 8822 29191 63450949
Premature rupture of membranes 102.76 27.21 35 8847 4958 63475182
Viral load increased 101.82 27.21 26 8856 1348 63478792
Renal colic 99.88 27.21 26 8856 1455 63478685
Nephrolithiasis 99.75 27.21 66 8816 41918 63438222
Immune reconstitution inflammatory syndrome 99.73 27.21 36 8846 6048 63474092
Cushing's syndrome 97.66 27.21 22 8860 665 63479475
Supernumerary nipple 96.61 27.21 15 8867 48 63480092
Low set ears 93.05 27.21 18 8864 252 63479888
Acoustic stimulation tests abnormal 90.30 27.21 15 8867 81 63480059
Renal dysplasia 88.36 27.21 17 8865 231 63479909
Low birth weight baby 87.05 27.21 34 8848 7095 63473045
Blood HIV RNA increased 80.18 27.21 19 8863 720 63479420
Lipodystrophy acquired 76.63 27.21 21 8861 1431 63478709
Congenital hydrocephalus 74.76 27.21 14 8868 163 63479977
Spina bifida 72.30 27.21 18 8864 841 63479299
Twin pregnancy 71.47 27.21 19 8863 1154 63478986
Blood bilirubin increased 70.80 27.21 51 8831 37089 63443051
Drug ineffective 67.84 27.21 31 8851 1044734 62435406
Drug resistance 66.75 27.21 41 8841 22892 63457248
Polydactyly 66.45 27.21 14 8868 307 63479833
Pre-eclampsia 66.01 27.21 30 8852 9103 63471037
Patent ductus arteriosus 65.38 27.21 24 8858 4226 63475914
Placenta praevia 64.36 27.21 17 8865 1007 63479133
Pain 64.09 27.21 13 8869 740615 62739525
Placental insufficiency 63.07 27.21 18 8864 1423 63478717
Adrenal suppression 61.24 27.21 16 8866 908 63479232
Pathogen resistance 59.17 27.21 25 8857 6373 63473767
Gestational diabetes 58.86 27.21 27 8855 8369 63471771
Blood bilirubin unconjugated increased 58.49 27.21 13 8869 369 63479771
Trisomy 21 58.05 27.21 13 8869 382 63479758
Premature labour 57.05 27.21 30 8852 12474 63467666
Single functional kidney 53.87 27.21 12 8870 344 63479796
Oligohydramnios 52.70 27.21 23 8859 6343 63473797
Genotype drug resistance test positive 51.53 27.21 12 8870 421 63479719
Trisomy 18 51.37 27.21 10 8872 145 63479995
Fanconi syndrome acquired 50.14 27.21 14 8868 1022 63479118
CD4 lymphocytes decreased 50.00 27.21 15 8867 1412 63478728
Renal tubular disorder 48.22 27.21 17 8865 2665 63477475
Polyhydramnios 47.04 27.21 16 8866 2255 63477885
Ultrasound antenatal screen abnormal 45.76 27.21 9 8873 138 63480002
Osteonecrosis 45.18 27.21 33 8849 24497 63455643
Renal aplasia 44.14 27.21 10 8872 310 63479830
Macrocephaly 43.47 27.21 8 8874 84 63480056
Congenital central nervous system anomaly 43.42 27.21 10 8872 334 63479806
Hydrocephalus 43.39 27.21 19 8863 5281 63474859
Fatigue 42.85 27.21 37 8845 887991 62592149
Foetal distress syndrome 42.32 27.21 13 8869 1325 63478815
Left ventricular dilatation 39.68 27.21 10 8872 491 63479649
Amniotic cavity infection 38.80 27.21 12 8870 1251 63478889
Eosinophilia 38.29 27.21 29 8853 22727 63457413
Coarctation of the aorta 38.25 27.21 10 8872 569 63479571
Fall 38.05 27.21 5 8877 392329 63087811
Microcephaly 37.83 27.21 11 8871 929 63479211
Calculus urinary 37.72 27.21 12 8870 1372 63478768
Ectopic pregnancy 37.65 27.21 14 8868 2553 63477587
Treatment noncompliance 36.86 27.21 35 8847 37290 63442850
Ocular icterus 36.20 27.21 15 8867 3641 63476499
Mitochondrial cytopathy 35.60 27.21 8 8874 239 63479901
Isoimmune haemolytic disease 35.44 27.21 6 8876 37 63480103
Hepatitis B DNA increased 34.80 27.21 8 8874 265 63479875
Joint swelling 34.76 27.21 3 8879 327663 63152477
Breast disorder 34.21 27.21 13 8869 2517 63477623
Dyspnoea 33.77 27.21 26 8856 661287 62818853
Alpha 1 foetoprotein abnormal 32.69 27.21 6 8876 62 63480078
Maternal drugs affecting foetus 31.02 27.21 15 8867 5227 63474913
Congenital anomaly 30.95 27.21 11 8871 1765 63478375
Foetal anaemia 30.27 27.21 6 8876 96 63480044
Encephalomalacia 30.10 27.21 8 8874 485 63479655
Congenital genital malformation female 30.10 27.21 5 8877 27 63480113
Hepatitis 29.57 27.21 32 8850 39756 63440384
Epidural lipomatosis 29.34 27.21 6 8876 113 63480027
Congenital skin dimples 29.19 27.21 6 8876 116 63480024
Oesophageal atresia 29.16 27.21 8 8874 547 63479593
Conduction disorder 29.07 27.21 10 8872 1457 63478683
Abdominal discomfort 29.01 27.21 5 8877 320880 63159260
Placental disorder 28.83 27.21 10 8872 1494 63478646
Subchorionic haematoma 28.77 27.21 6 8876 125 63480015
Placental chorioangioma 28.73 27.21 4 8878 4 63480136
Cerebral ventricle dilatation 28.37 27.21 9 8873 1020 63479120
Swelling 27.94 27.21 3 8879 275375 63204765
Cholestasis 27.92 27.21 27 8855 29407 63450733

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
Drug interaction 1555.48 17.34 1087 15703 224859 34715282
Depression 1511.68 17.34 791 15999 96307 34843834
Nephrolithiasis 442.89 17.34 238 16552 30095 34910046
Hyperbilirubinaemia 412.48 17.34 188 16602 16655 34923486
Foetal exposure during pregnancy 405.25 17.34 243 16547 37858 34902283
Lipodystrophy acquired 386.74 17.34 117 16673 3227 34936914
Psychiatric decompensation 384.10 17.34 113 16677 2824 34937317
Depression suicidal 339.10 17.34 99 16691 2406 34937735
Loss of personal independence in daily activities 335.66 17.34 205 16585 32974 34907167
Tearfulness 328.62 17.34 98 16692 2569 34937572
Renal colic 327.27 17.34 90 16700 1749 34938392
Depressive symptom 279.70 17.34 88 16702 2771 34937370
Jaundice 250.41 17.34 168 16622 31714 34908427
Psychomotor skills impaired 241.23 17.34 85 16705 3821 34936320
Renal tubular disorder 212.40 17.34 81 16709 4562 34935579
Paranoia 208.16 17.34 106 16684 11962 34928179
Mitochondrial toxicity 175.33 17.34 61 16729 2638 34937503
Blood bilirubin increased 169.13 17.34 143 16647 38153 34901988
Psychotic disorder 166.34 17.34 118 16672 24334 34915807
Immune reconstitution inflammatory syndrome 157.06 17.34 79 16711 8680 34931461
Fanconi syndrome acquired 152.83 17.34 51 16739 1940 34938201
Suicidal ideation 146.71 17.34 135 16655 40253 34899888
Virologic failure 138.91 17.34 55 16735 3425 34936716
Eyelid ptosis 130.50 17.34 61 16729 5705 34934436
Calculus urinary 119.88 17.34 39 16751 1368 34938773
Psychomotor retardation 119.35 17.34 50 16740 3600 34936541
Ocular icterus 103.11 17.34 42 16748 2815 34937326
Lipoatrophy 95.50 17.34 26 16764 485 34939656
Blood HIV RNA increased 88.44 17.34 30 16760 1200 34938941
Viral mutation identified 88.39 17.34 38 16752 2916 34937225
Blood bilirubin unconjugated increased 86.07 17.34 25 16765 595 34939546
HIV-associated neurocognitive disorder 85.79 17.34 22 16768 322 34939819
Premature baby 83.91 17.34 72 16718 19561 34920580
Trisomy 21 82.96 17.34 24 16766 563 34939578
Viral load increased 80.56 17.34 34 16756 2493 34937648
Osteonecrosis 76.99 17.34 61 16729 14829 34925312
Fanconi syndrome 75.04 17.34 29 16761 1691 34938450
Heterotaxia 73.06 17.34 16 16774 112 34940029
Cushing's syndrome 67.89 17.34 19 16771 394 34939747
Death 65.75 17.34 57 16733 397992 34542149
Proteinuria 65.08 17.34 61 16729 18581 34921560
Diplopia 64.42 17.34 58 16732 16785 34923356
CD4 lymphocytes decreased 64.22 17.34 26 16764 1715 34938426
Single umbilical artery 64.08 17.34 16 16774 209 34939932
Kaposi's sarcoma 61.39 17.34 21 16769 862 34939279
Cholelithiasis 58.59 17.34 61 16729 21087 34919054
Drug ineffective 58.25 17.34 81 16709 456670 34483471
Glycosuria 58.07 17.34 22 16768 1215 34938926
Off label use 58.01 17.34 70 16720 419454 34520687
Osteoporosis 57.28 17.34 48 16742 12620 34927521
Prescribed overdose 53.72 17.34 43 16747 10604 34929537
Pathogen resistance 53.69 17.34 41 16749 9441 34930700
Pulmonary haemorrhage neonatal 53.54 17.34 9 16781 9 34940132
Anxiety 47.14 17.34 129 16661 99299 34840842
Periventricular leukomalacia 46.30 17.34 10 16780 65 34940076
Cortisol decreased 45.63 17.34 18 16772 1109 34939032
Ureterolithiasis 45.49 17.34 22 16768 2217 34937924
Nephropathy toxic 45.49 17.34 42 16748 12546 34927595
Hypotension 45.44 17.34 25 16765 221624 34718517
Chordee 45.05 17.34 10 16780 75 34940066
Drug resistance 43.75 17.34 58 16732 25869 34914272
Blood antidiuretic hormone increased 43.35 17.34 9 16781 47 34940094
Hypertriglyceridaemia 42.36 17.34 34 16756 8414 34931727
Fall 41.41 17.34 23 16767 202862 34737279
Pneumonia 40.69 17.34 70 16720 362557 34577584
Nephrocalcinosis 39.60 17.34 14 16776 634 34939507
Febrile neutropenia 38.93 17.34 9 16781 136840 34803301
Disease progression 37.73 17.34 4 16786 108073 34832068
Dyspnoea 37.64 17.34 78 16712 376704 34563437
Acquired immunodeficiency syndrome 34.77 17.34 12 16778 506 34939635
Exposure during pregnancy 34.61 17.34 31 16759 8903 34931238
Neonatal hyponatraemia 33.99 17.34 8 16782 80 34940061
Hepatitis C 33.98 17.34 32 16758 9798 34930343
HIV wasting syndrome 33.47 17.34 8 16782 86 34940055
Vanishing bile duct syndrome 33.46 17.34 14 16776 1004 34939137
Congenital hydrocephalus 33.13 17.34 8 16782 90 34940051
Wrong dose 33.06 17.34 12 16778 587 34939554
Adrenal suppression 32.16 17.34 12 16778 635 34939506
CSF HIV escape syndrome 31.91 17.34 9 16781 192 34939949
Foetal chromosome abnormality 31.80 17.34 6 16784 17 34940124
Congenital naevus 31.54 17.34 6 16784 18 34940123
Hypophosphataemia 30.88 17.34 32 16758 10994 34929147
Hypothalamic pituitary adrenal axis suppression 29.91 17.34 8 16782 139 34940002
White matter lesion 29.48 17.34 12 16778 802 34939339
Anomalous pulmonary venous connection 29.30 17.34 7 16783 75 34940066
Crystal urine 29.30 17.34 7 16783 75 34940066
CSF virus identified 29.11 17.34 6 16784 30 34940111
Enanthema 29.05 17.34 10 16780 418 34939723
Completed suicide 28.83 17.34 6 16784 98162 34841979
Dysphagia 28.61 17.34 80 16710 62301 34877840
Hepatitis 27.98 17.34 45 16745 23859 34916282
Low birth weight baby 27.83 17.34 26 16764 7879 34932262
Trimethylaminuria 27.72 17.34 5 16785 10 34940131
Blood pressure increased 26.68 17.34 5 16785 88097 34852044
Hepatic cirrhosis 26.57 17.34 37 16753 17277 34922864
Biliary colic 26.41 17.34 12 16778 1050 34939091
Alpha 1 foetoprotein abnormal 26.28 17.34 5 16785 15 34940126
Constipation 25.86 17.34 17 16773 136965 34803176
Alanine aminotransferase increased 25.43 17.34 91 16699 80724 34859417
Hydronephrosis 25.40 17.34 28 16762 10318 34929823
Drug abuse 25.38 17.34 8 16782 99088 34841053
Sepsis 24.87 17.34 26 16764 166535 34773606
Renal failure 24.75 17.34 126 16664 130431 34809710
Cardiac failure congestive 24.64 17.34 5 16785 83265 34856876
Haemophilic arthropathy 24.41 17.34 7 16783 159 34939982
Intraventricular haemorrhage neonatal 23.95 17.34 8 16782 305 34939836
Persistent left superior vena cava 23.80 17.34 4 16786 4 34940137
Neonatal seizure 23.79 17.34 9 16781 495 34939646
Intestinal malrotation 23.49 17.34 5 16785 30 34940111
Atrial fibrillation 23.36 17.34 15 16775 122378 34817763
Hyperbilirubinaemia neonatal 23.20 17.34 10 16780 772 34939369
Genotype drug resistance test positive 22.51 17.34 11 16779 1134 34939007
Tubulointerstitial nephritis 22.48 17.34 38 16752 20986 34919155
Jarisch-Herxheimer reaction 22.40 17.34 9 16781 582 34939559
Anogenital warts 22.31 17.34 9 16781 588 34939553
Cardiac failure 22.26 17.34 8 16782 91240 34848901
Infection 22.13 17.34 8 16782 90907 34849234
Genitalia external ambiguous 22.12 17.34 7 16783 224 34939917
Heart transplant rejection 21.75 17.34 11 16779 1220 34938921
Pain 21.55 17.34 41 16749 204634 34735507
Umbilical cord abnormality 21.52 17.34 5 16785 47 34940094
Hyperadrenocorticism 21.50 17.34 6 16784 123 34940018
Renal tubular dysfunction 21.43 17.34 8 16782 424 34939717
Cough 20.70 17.34 25 16765 150115 34790026
Adrenogenital syndrome 20.41 17.34 5 16785 60 34940081
Facial wasting 20.34 17.34 6 16784 151 34939990
Encephalitis 20.16 17.34 21 16769 7256 34932885
Peripheral swelling 19.92 17.34 6 16784 76535 34863606
Ventricular septal defect 19.84 17.34 16 16774 3985 34936156
Product dose omission issue 19.83 17.34 17 16773 119694 34820447
Acute stress disorder 19.63 17.34 6 16784 171 34939970
Portal fibrosis 19.61 17.34 7 16783 326 34939815
Right aortic arch 19.41 17.34 4 16786 20 34940121
Hyperlipidaemia 19.30 17.34 29 16761 14500 34925641
Congenital hepatomegaly 19.25 17.34 4 16786 21 34940120
Mitochondrial cytopathy 19.15 17.34 6 16784 186 34939955
Mycobacterium avium complex infection 19.12 17.34 13 16777 2498 34937643
Encephalitis viral 19.02 17.34 10 16780 1202 34938939
Thalassaemia alpha 18.52 17.34 4 16786 26 34940115
Erythema elevatum diutinum 18.52 17.34 4 16786 26 34940115
Blood triglycerides increased 18.44 17.34 28 16762 14131 34926010
Depressed mood 18.17 17.34 33 16757 19284 34920857
Deafness congenital 17.99 17.34 5 16785 101 34940040
Pancreatitis 17.94 17.34 50 16740 38841 34901300
Polymicrogyria 17.85 17.34 3 16787 3 34940138
Foetal monitoring abnormal 17.85 17.34 3 16787 3 34940138
Foetal cystic hygroma 17.85 17.34 3 16787 3 34940138
White blood cell count decreased 17.79 17.34 12 16778 95433 34844708
Ophthalmoplegia 17.62 17.34 11 16779 1829 34938312
Chest pain 17.58 17.34 21 16769 126741 34813400
Incorrect route of product administration 17.44 17.34 28 16762 14817 34925324
Drug level increased 17.40 17.34 35 16755 22061 34918080
Anal cancer 17.37 17.34 7 16783 456 34939685

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
Drug interaction 1467.76 18.06 1026 18544 414157 79310661
Depression 934.30 18.06 608 18962 216182 79508636
Abortion spontaneous 856.66 18.06 308 19262 29199 79695619
Hyperbilirubinaemia 575.37 18.06 219 19351 24299 79700519
Maternal exposure during pregnancy 519.09 18.06 355 19215 136183 79588635
Lipodystrophy acquired 501.34 18.06 131 19439 4194 79720624
Nephrolithiasis 461.08 18.06 236 19334 53055 79671763
Psychiatric decompensation 425.63 18.06 113 19457 3850 79720968
Depression suicidal 358.28 18.06 98 19472 3744 79721074
Abortion induced 331.36 18.06 106 19464 7003 79717815
Jaundice 324.12 18.06 187 19383 53162 79671656
Tearfulness 314.40 18.06 98 19472 5947 79718871
Renal colic 300.67 18.06 80 19490 2747 79722071
Psychomotor skills impaired 276.96 18.06 86 19484 5151 79719667
Exposure during pregnancy 270.61 18.06 213 19357 100919 79623899
Depressive symptom 263.71 18.06 87 19483 6336 79718482
Stillbirth 256.52 18.06 76 19494 3879 79720939
Immune reconstitution inflammatory syndrome 248.67 18.06 102 19468 13739 79711079
Loss of personal independence in daily activities 240.46 18.06 200 19370 102380 79622438
Paranoia 230.89 18.06 107 19463 19325 79705493
Viral mutation identified 227.99 18.06 69 19501 3789 79721029
Renal tubular disorder 223.42 18.06 77 19493 6409 79718409
Mitochondrial toxicity 220.25 18.06 64 19506 3050 79721768
Virologic failure 213.97 18.06 67 19503 4124 79720694
Blood bilirubin increased 193.40 18.06 147 19423 66085 79658733
Caesarean section 180.64 18.06 79 19491 12456 79712362
Premature delivery 177.26 18.06 95 19475 23372 79701446
Fanconi syndrome acquired 175.71 18.06 52 19518 2642 79722176
Psychotic disorder 172.05 18.06 114 19456 41288 79683530
Live birth 167.68 18.06 85 19485 18659 79706159
Pregnancy 165.29 18.06 95 19475 26756 79698062
Viral load increased 162.57 18.06 50 19520 2898 79721920
Suicidal ideation 142.83 18.06 131 19439 76209 79648609
Calculus urinary 136.83 18.06 42 19528 2418 79722400
Eyelid ptosis 134.87 18.06 62 19508 10982 79713836
Pathogen resistance 134.03 18.06 67 19503 14275 79710543
Blood bilirubin unconjugated increased 132.71 18.06 34 19536 1003 79723815
Cushing's syndrome 129.18 18.06 33 19537 962 79723856
Psychomotor retardation 119.37 18.06 48 19522 6136 79718682
Blood HIV RNA increased 114.00 18.06 34 19536 1774 79723044
Foetal death 113.63 18.06 50 19520 7994 79716824
Pregnancy on contraceptive 107.37 18.06 28 19542 887 79723931
Osteonecrosis 106.44 18.06 76 19494 31019 79693799
Drug resistance 104.41 18.06 85 19485 42128 79682690
Ocular icterus 103.78 18.06 42 19528 5458 79719360
Foetal exposure during pregnancy 98.31 18.06 41 19529 5749 79719069
Adrenal suppression 95.60 18.06 28 19542 1371 79723447
CD4 lymphocytes decreased 93.54 18.06 32 19538 2602 79722216
Fanconi syndrome 91.00 18.06 32 19538 2824 79721994
CSF HIV escape syndrome 83.84 18.06 19 19551 328 79724490
HIV-associated neurocognitive disorder 78.20 18.06 18 19552 334 79724484
Normal newborn 77.97 18.06 37 19533 7035 79717783
Genotype drug resistance test positive 75.59 18.06 23 19547 1285 79723533
Drug ineffective 75.56 18.06 93 19477 1080820 78643998
Proteinuria 75.25 18.06 63 19507 32439 79692379
Lipoatrophy 70.89 18.06 19 19551 670 79724148
Premature rupture of membranes 69.71 18.06 29 19541 4040 79720778
Pain 67.61 18.06 45 19525 703757 79021061
Twin pregnancy 65.95 18.06 19 19551 877 79723941
Nephropathy toxic 65.52 18.06 48 19522 20371 79704447
Diplopia 61.70 18.06 57 19513 33409 79691409
Osteoporosis 61.39 18.06 71 19499 54041 79670777
Glycosuria 60.23 18.06 22 19548 2166 79722652
Fall 57.34 18.06 24 19546 487605 79237213
Placenta praevia 55.53 18.06 16 19554 739 79724079
Hypertriglyceridaemia 55.12 18.06 36 19534 12704 79712114
Hepatitis 54.82 18.06 68 19502 55659 79669159
Renal failure 53.51 18.06 138 19432 200830 79523988
Cortisol decreased 53.04 18.06 20 19550 2152 79722666
Pre-eclampsia 51.73 18.06 28 19542 7013 79717805
Cholelithiasis 51.38 18.06 64 19506 52600 79672218
Dyspnoea 49.64 18.06 84 19486 856941 78867877
Renal tubular dysfunction 46.34 18.06 14 19556 763 79724055
Mitochondrial cytopathy 45.48 18.06 12 19558 398 79724420
Off label use 45.45 18.06 97 19473 907118 78817700
Acquired immunodeficiency syndrome 43.90 18.06 11 19559 296 79724522
Peripheral swelling 43.53 18.06 7 19563 269610 79455208
Joint swelling 43.37 18.06 9 19561 288637 79436181
Ureterolithiasis 42.01 18.06 20 19550 3828 79720990
Hypophosphataemia 40.80 18.06 36 19534 19877 79704941
Secondary adrenocortical insufficiency 40.20 18.06 18 19552 2996 79721822
Blood antidiuretic hormone increased 40.00 18.06 8 19562 73 79724745
Acute kidney injury 39.66 18.06 240 19330 519164 79205654
Abdominal discomfort 39.39 18.06 7 19563 250720 79474098
Polyhydramnios 38.99 18.06 15 19555 1705 79723113
Treatment noncompliance 37.94 18.06 55 19515 52213 79672605
Infection 37.43 18.06 7 19563 241705 79483113
Placental insufficiency 37.38 18.06 13 19557 1110 79723708
Amniotic cavity infection 37.16 18.06 12 19558 815 79724003
Swelling 36.42 18.06 5 19565 216706 79508112
Hypotension 36.06 18.06 33 19537 440284 79284534
Renal dysplasia 35.94 18.06 7 19563 55 79724763
Spina bifida 35.04 18.06 8 19562 143 79724675
Vanishing bile duct syndrome 35.00 18.06 14 19556 1764 79723054
HIV wasting syndrome 34.51 18.06 7 19563 69 79724749
Prescribed overdose 33.73 18.06 44 19526 37839 79686979
Nephrocalcinosis 33.69 18.06 13 19557 1489 79723329
Hypothalamic pituitary adrenal axis suppression 33.35 18.06 9 19561 326 79724492
Gestational diabetes 32.78 18.06 20 19550 6273 79718545
Anxiety 32.61 18.06 134 19436 248378 79476440
CSF virus identified 32.21 18.06 6 19564 36 79724782
Cough 31.83 18.06 26 19544 366763 79358055
Constipation 31.55 18.06 15 19555 283035 79441783
Premature baby 30.50 18.06 16 19554 3764 79721054
Arthralgia 30.38 18.06 59 19511 571744 79153074
Tubulointerstitial nephritis 30.36 18.06 42 19528 38193 79686625
Ergot poisoning 30.11 18.06 7 19563 136 79724682
Hepatitis B DNA increased 29.32 18.06 10 19560 805 79724013
Acute HIV infection 29.07 18.06 6 19564 65 79724753
Syphilis 28.87 18.06 9 19561 545 79724273
Wrong dose 28.77 18.06 12 19558 1682 79723136
Blood corticotrophin decreased 28.71 18.06 9 19561 555 79724263
COVID-19 28.06 18.06 3 19567 157671 79567147
Placental disorder 28.00 18.06 10 19560 923 79723895
Death 27.93 18.06 61 19509 566453 79158365
Pneumonia 27.93 18.06 77 19493 660169 79064649
Nasopharyngitis 27.46 18.06 14 19556 253867 79470951
Alanine aminotransferase increased 27.40 18.06 95 19475 162475 79562343
Hepatitis C 27.36 18.06 23 19547 11902 79712916
Condition aggravated 27.22 18.06 51 19519 501073 79223745
Disease progression 27.16 18.06 6 19564 184356 79540462
Product use issue 26.84 18.06 9 19561 209813 79515005
Placental chorioangioma 26.48 18.06 4 19566 4 79724814
Subchorionic haematoma 26.13 18.06 6 19564 110 79724708
Febrile neutropenia 26.11 18.06 12 19558 230987 79493831
Kaposi's sarcoma 26.09 18.06 9 19561 750 79724068
Cholestasis 25.70 18.06 46 19524 52063 79672755
Dysphagia 25.68 18.06 77 19493 122059 79602759
Crystal urine 25.41 18.06 6 19564 125 79724693
Single functional kidney 25.12 18.06 7 19563 286 79724532
Renal aplasia 25.10 18.06 6 19564 132 79724686
Mycobacterium avium complex infection 24.94 18.06 15 19555 4585 79720233
Product dose omission issue 24.82 18.06 15 19555 247522 79477296
Bilirubin conjugated increased 24.81 18.06 16 19554 5523 79719295
Urinary tract infection 24.38 18.06 19 19551 274493 79450325
Foetal exposure during delivery 24.24 18.06 4 19566 10 79724808
Jarisch-Herxheimer reaction 24.05 18.06 9 19561 948 79723870
Encephalitis viral 23.94 18.06 12 19558 2567 79722251
Blood pressure increased 23.85 18.06 11 19559 211349 79513469
Cholestasis of pregnancy 23.73 18.06 9 19561 984 79723834
Conduction disorder 23.61 18.06 13 19557 3366 79721452
Alpha 1 foetoprotein abnormal 23.53 18.06 5 19565 63 79724755
Hepatic cytolysis 23.34 18.06 31 19539 27120 79697698
Toxic skin eruption 23.20 18.06 28 19542 22265 79702553
Encephalitis 23.15 18.06 23 19547 14737 79710081
Premature labour 23.09 18.06 18 19552 8372 79716446
Renal impairment 23.03 18.06 88 19482 157695 79567123
Erythema elevatum diutinum 22.82 18.06 4 19566 16 79724802
Congenital hydrocephalus 22.60 18.06 5 19565 77 79724741
Blood lactic acid increased 22.13 18.06 21 19549 12723 79712095
Ectopic pregnancy 21.95 18.06 10 19560 1733 79723085
Alopecia 21.86 18.06 15 19555 231340 79493478
Completed suicide 21.83 18.06 17 19553 245750 79479068
Myoglobin blood increased 21.68 18.06 12 19558 3139 79721679
Hydronephrosis 21.65 18.06 24 19546 17430 79707388
Blood creatinine increased 21.42 18.06 85 19485 154972 79569846
Enanthema 21.39 18.06 8 19562 841 79723977
Drug intolerance 21.35 18.06 20 19550 264099 79460719
ACTH stimulation test abnormal 21.33 18.06 4 19566 25 79724793
Lipohypertrophy 21.08 18.06 8 19562 876 79723942
Oligohydramnios 20.79 18.06 12 19558 3400 79721418
Adrenal insufficiency 20.70 18.06 30 19540 28457 79696361
Retinal toxicity 20.67 18.06 9 19561 1402 79723416
Inappropriate schedule of product administration 20.40 18.06 4 19566 133624 79591194
Placental infarction 20.31 18.06 5 19565 125 79724693
Seborrhoeic dermatitis 20.30 18.06 10 19560 2063 79722755
Cardiac failure congestive 20.25 18.06 5 19565 142397 79582421
Pancreatitis 20.22 18.06 49 19521 68526 79656292
Cytomegalovirus chorioretinitis 20.13 18.06 14 19556 5476 79719342
Gynaecomastia 20.11 18.06 16 19554 7665 79717153
Portal fibrosis 19.94 18.06 7 19563 614 79724204
Musculoskeletal stiffness 19.91 18.06 9 19561 174999 79549819
Pain in extremity 19.87 18.06 37 19533 364501 79360317
Atrial fibrillation 19.82 18.06 12 19558 197874 79526944
Ophthalmoplegia 19.79 18.06 11 19559 2901 79721917
Haemolytic anaemia 19.56 18.06 23 19547 17797 79707021
Hyperadrenocorticism 19.45 18.06 6 19564 351 79724467
Drug hypersensitivity 19.43 18.06 27 19543 298889 79425929
Depressed mood 19.22 18.06 39 19531 48441 79676377
Cerebral toxoplasmosis 19.06 18.06 10 19560 2352 79722466
Hepatic cirrhosis 18.75 18.06 32 19538 34874 79689944
Craniofacial deformity 18.64 18.06 3 19567 6 79724812
Hyperproteinaemia 18.64 18.06 5 19565 177 79724641
Arthritis 18.49 18.06 3 19567 114877 79609941
Aspartate aminotransferase increased 18.35 18.06 75 19495 138566 79586252
Trimethylaminuria 18.27 18.06 5 19565 191 79724627
Nasal septum deviation 18.23 18.06 9 19561 1864 79722954
Acute stress disorder 18.16 18.06 6 19564 438 79724380

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AE08 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Protease inhibitors
ATC J05AR15 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR23 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
FDA MoA N0000000246 HIV Protease Inhibitors
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 D017320 HIV Protease Inhibitors
MeSH PA D011480 Protease Inhibitors
MeSH PA D000084762 Viral Protease Inhibitors
FDA EPC N0000175889 Protease Inhibitor
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
FDA MoA N0000191269 UDP Glucuronosyltransferases Inhibitors
FDA MoA N0000191272 UGT1A1 Inhibitors
CHEBI has role CHEBI:35660 HIV protease inhibitors
CHEBI has role CHEBI:36044 antiviral drugs

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
Hyperbilirubinemia contraindication 14783006 DOID:2741
Hepatic failure contraindication 59927004
Chronic type B viral hepatitis contraindication 61977001
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Hemophilia contraindication 90935002
Lactic acidosis contraindication 91273001 DOID:3650
Kidney stone contraindication 95570007
Chronic hepatitis C contraindication 128302006
Liver function tests abnormal contraindication 166603001
Atrioventricular block contraindication 233917008 DOID:0050820
Disease of liver contraindication 235856003 DOID:409
Breastfeeding (mother) contraindication 413712001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.91 acidic
pKa2 11.57 acidic
pKa3 4.94 Basic
pKa4 1.0 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 300MG BASE;150MG EVOTAZ BRISTOL N206353 Jan. 29, 2015 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Multidrug resistance protein 1 Transporter IC50 4.17 CHEMBL
ATP-binding cassette sub-family G member 2 Transporter IC50 4.16 CHEMBL
Cytochrome P450 2C9 Enzyme Ki 4.92 WOMBAT-PK
Cytochrome P450 1A2 Enzyme Ki 4.92 WOMBAT-PK
UDP-glucuronosyltransferase 1-1 Enzyme Ki 5.72 WOMBAT-PK
Cytochrome P450 3A4 Enzyme Ki 5.63 WOMBAT-PK
Pol polyprotein Enzyme INHIBITOR Ki 9.62 CHEMBL CHEMBL
Gag-Pol polyprotein Polyprotein Ki 8.58 WOMBAT-PK
Reverse transcriptase/RNaseH Enzyme IC50 7.59 CHEMBL
Protease Enzyme IC50 8.40 CHEMBL
Protease Unclassified Ki 10.27 CHEMBL
Protease Unclassified Ki 10.12 CHEMBL

External reference:

IDSource
4024316 VUID
N0000022320 NUI
D01276 KEGG_DRUG
229975-97-7 SECONDARY_CAS_RN
343047 RXNORM
C1176383 UMLSCUI
CHEBI:37924 CHEBI
DR7 PDB_CHEM_ID
CHEMBL1163 ChEMBL_ID
CHEMBL1200678 ChEMBL_ID
D000069446 MESH_DESCRIPTOR_UI
DB01072 DRUGBANK_ID
11138 IUPHAR_LIGAND_ID
8181 INN_ID
QZU4H47A3S UNII
148192 PUBCHEM_CID
17380 MMSL
267545 MMSL
30601 MMSL
46998 MMSL
d04882 MMSL
404838006 SNOMEDCT_US
413591007 SNOMEDCT_US
413592000 SNOMEDCT_US
4021397 VANDF
4024316 VANDF
000306 NDDF
000539 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
REYATAZ HUMAN PRESCRIPTION DRUG LABEL 1 0003-3622 CAPSULE, GELATIN COATED 300 mg ORAL NDA 29 sections
REYATAZ HUMAN PRESCRIPTION DRUG LABEL 1 0003-3622 CAPSULE, GELATIN COATED 300 mg ORAL NDA 29 sections
REYATAZ HUMAN PRESCRIPTION DRUG LABEL 1 0003-3624 CAPSULE, GELATIN COATED 150 mg ORAL NDA 29 sections
REYATAZ HUMAN PRESCRIPTION DRUG LABEL 1 0003-3624 CAPSULE, GELATIN COATED 150 mg ORAL NDA 29 sections
REYATAZ HUMAN PRESCRIPTION DRUG LABEL 1 0003-3631 CAPSULE, GELATIN COATED 200 mg ORAL NDA 29 sections
REYATAZ HUMAN PRESCRIPTION DRUG LABEL 1 0003-3631 CAPSULE, GELATIN COATED 200 mg ORAL NDA 29 sections
REYATAZ HUMAN PRESCRIPTION DRUG LABEL 1 0003-3638 POWDER 50 mg ORAL NDA 29 sections
REYATAZ HUMAN PRESCRIPTION DRUG LABEL 1 0003-3638 POWDER 50 mg ORAL NDA 29 sections
EVOTAZ HUMAN PRESCRIPTION DRUG LABEL 2 0003-3641 TABLET 300 mg ORAL NDA 30 sections
EVOTAZ HUMAN PRESCRIPTION DRUG LABEL 2 0003-3641 TABLET 300 mg ORAL NDA 30 sections
EVOTAZ HUMAN PRESCRIPTION DRUG LABEL 2 0003-3641 TABLET 300 mg ORAL NDA 30 sections
Atazanavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5526 CAPSULE 150 mg ORAL ANDA 28 sections
Atazanavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5526 CAPSULE 150 mg ORAL ANDA 28 sections
Atazanavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5526 CAPSULE 150 mg ORAL ANDA 28 sections
Atazanavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5527 CAPSULE 200 mg ORAL ANDA 28 sections
Atazanavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5527 CAPSULE 200 mg ORAL ANDA 28 sections
Atazanavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5527 CAPSULE 200 mg ORAL ANDA 28 sections
Atazanavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5528 CAPSULE 300 mg ORAL ANDA 28 sections
Atazanavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5528 CAPSULE 300 mg ORAL ANDA 28 sections
Atazanavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5528 CAPSULE 300 mg ORAL ANDA 28 sections
Atazanavir Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 0904-6875 CAPSULE 300 mg ORAL ANDA 27 sections
Atazanavir Sulfate Human Prescription Drug Label 1 16714-860 CAPSULE 150 mg ORAL ANDA 27 sections
Atazanavir Sulfate Human Prescription Drug Label 1 16714-860 CAPSULE 150 mg ORAL ANDA 27 sections
Atazanavir Sulfate Human Prescription Drug Label 1 16714-861 CAPSULE 200 mg ORAL ANDA 27 sections
Atazanavir Sulfate Human Prescription Drug Label 1 16714-861 CAPSULE 200 mg ORAL ANDA 27 sections
Atazanavir Sulfate Human Prescription Drug Label 1 16714-862 CAPSULE 300 mg ORAL ANDA 27 sections
Atazanavir Sulfate Human Prescription Drug Label 1 16714-862 CAPSULE 300 mg ORAL ANDA 27 sections
Atazanavir HUMAN PRESCRIPTION DRUG LABEL 1 31722-653 CAPSULE 150 mg ORAL ANDA 29 sections
Atazanavir HUMAN PRESCRIPTION DRUG LABEL 1 31722-654 CAPSULE 200 mg ORAL ANDA 29 sections
Atazanavir HUMAN PRESCRIPTION DRUG LABEL 1 31722-655 CAPSULE 300 mg ORAL ANDA 29 sections