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

Stem definitionDrug idCAS RN
antivirals 2352 518048-05-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • MK0518
  • isentress
  • raltegravir
  • raltegravir potassium
  • MK-0518
Raltegravir inhibits the catalytic activity of HIV-1 integrase, an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the covalent insertion, or integration, of unintegrated linear HIV-1 DNA into the host cell genome preventing the formation of the HIV-1 provirus. The provirus is required to direct the production of progeny virus, so inhibiting integration prevents propagation of the viral infection.
  • Molecular weight: 444.42
  • Formula: C20H21FN6O5
  • CLOGP: 1.47
  • LIPINSKI: 1
  • HAC: 11
  • HDO: 3
  • TPSA: 150.02
  • ALOGS: -3.66
  • ROTB: 6

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.80 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 9 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 25.72 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 31.80 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
June 24, 2008 PMDA Banyu Pharmaceutical Co., Ltd.
Dec. 20, 2007 EMA
Oct. 12, 2007 FDA MERCK SHARP DOHME

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Exposure during pregnancy 1176.15 23.10 526 8738 120489 50475371
Foetal exposure during pregnancy 578.09 23.10 209 9055 27150 50568710
Maternal exposure during pregnancy 305.36 23.10 244 9020 159534 50436326
Abortion spontaneous 261.11 23.10 135 9129 41637 50554223
Virologic failure 245.20 23.10 57 9207 1507 50594353
Premature baby 226.39 23.10 95 9169 18242 50577618
Immune reconstitution inflammatory syndrome 190.37 23.10 61 9203 5455 50590405
Blood HIV RNA increased 141.11 23.10 30 9234 519 50595341
Pathogen resistance 140.88 23.10 49 9215 5640 50590220
Lipodystrophy acquired 139.22 23.10 35 9229 1294 50594566
Drug reaction with eosinophilia and systemic symptoms 130.58 23.10 75 9189 28349 50567511
Premature delivery 126.56 23.10 69 9195 23594 50572266
Viral load increased 123.67 23.10 31 9233 1132 50594728
Viral mutation identified 122.67 23.10 33 9231 1596 50594264
Premature labour 113.89 23.10 51 9213 11425 50584435
Caesarean section 113.53 23.10 56 9208 15583 50580277
Spina bifida 107.11 23.10 25 9239 672 50595188
Ectopic kidney 98.10 23.10 16 9248 54 50595806
Abortion induced 97.45 23.10 43 9221 9301 50586559
Live birth 88.14 23.10 48 9216 16360 50579500
Foetal growth restriction 87.33 23.10 36 9228 6591 50589269
Treatment noncompliance 86.46 23.10 59 9205 30091 50565769
Sudden infant death syndrome 86.45 23.10 17 9247 195 50595665
Cloacal exstrophy 84.60 23.10 16 9248 147 50595713
Foetal death 80.03 23.10 36 9228 8144 50587716
Congenital genital malformation 79.49 23.10 15 9249 136 50595724
Bladder agenesis 79.00 23.10 15 9249 141 50595719
Drug resistance 78.98 23.10 47 9217 18942 50576918
Genitalia external ambiguous 78.34 23.10 15 9249 148 50595712
Caudal regression syndrome 77.36 23.10 15 9249 159 50595701
Meconium stain 75.66 23.10 15 9249 180 50595680
Gastrointestinal disorder congenital 74.28 23.10 14 9250 126 50595734
Tethered cord syndrome 72.87 23.10 15 9249 220 50595640
Anal atresia 70.64 23.10 16 9248 375 50595485
Meningomyelocele 69.68 23.10 17 9247 554 50595306
Congenital heart valve disorder 68.68 23.10 12 9252 67 50595793
Premature rupture of membranes 67.62 23.10 27 9237 4553 50591307
Neonatal respiratory arrest 65.98 23.10 11 9253 44 50595816
Gastrointestinal malformation 64.40 23.10 13 9251 172 50595688
Hepatocellular injury 63.29 23.10 46 9218 25901 50569959
Gastroschisis 60.55 23.10 13 9251 236 50595624
Exomphalos 60.09 23.10 15 9249 538 50595322
Congenital pulmonary valve disorder 59.21 23.10 10 9254 44 50595816
Umbilical cord abnormality 58.80 23.10 15 9249 588 50595272
Immune reconstitution inflammatory syndrome associated tuberculosis 56.82 23.10 13 9251 319 50595541
Hemivertebra 56.61 23.10 11 9253 118 50595742
Complication of delivery 55.03 23.10 11 9253 138 50595722
Congenital anomaly 53.19 23.10 17 9247 1504 50594356
Maternal drugs affecting foetus 51.76 23.10 23 9241 5054 50590806
Pulmonary valve sclerosis 48.60 23.10 8 9256 29 50595831
Pain 48.21 23.10 23 9241 578880 50016980
CD4 lymphocytes decreased 46.97 23.10 15 9249 1324 50594536
Neural tube defect 46.55 23.10 10 9254 182 50595678
Congenital choroid plexus cyst 46.48 23.10 11 9253 314 50595546
Generalised anxiety disorder 46.29 23.10 16 9248 1804 50594056
Congenital ectopic bladder 46.20 23.10 9 9255 98 50595762
Hyperbilirubinaemia 45.92 23.10 26 9238 9544 50586316
Cardiac murmur 45.63 23.10 27 9237 10757 50585103
Anencephaly 45.47 23.10 10 9254 204 50595656
Stillbirth 45.23 23.10 22 9242 5930 50589930
Drug interaction 44.77 23.10 107 9157 199514 50396346
Congenital hydrocephalus 43.65 23.10 9 9255 133 50595727
Drug ineffective 43.43 23.10 52 9212 819281 49776579
Genotype drug resistance test positive 42.44 23.10 10 9254 280 50595580
Cholestasis of pregnancy 41.03 23.10 13 9251 1118 50594742
Renal tubular dysfunction 39.94 23.10 10 9254 363 50595497
Low birth weight baby 39.53 23.10 20 9244 5861 50589999
Fall 39.28 23.10 7 9257 334925 50260935
Pre-eclampsia 38.98 23.10 22 9242 8022 50587838
Gestational diabetes 37.76 23.10 21 9243 7444 50588416
Mycoplasma genitalium infection 37.32 23.10 6 9258 18 50595842
Product size issue 36.63 23.10 9 9255 302 50595558
Viral load decreased 35.79 23.10 6 9258 25 50595835
Hepatitis fulminant 34.85 23.10 15 9249 3053 50592807
Hydrocephalus 34.30 23.10 17 9247 4771 50591089
Ventricular hypertrophy 34.17 23.10 15 9249 3200 50592660
Central obesity 34.01 23.10 11 9253 1011 50594849
Sepsis neonatal 33.74 23.10 9 9255 421 50595439
Oesophageal candidiasis 33.62 23.10 17 9247 4977 50590883
Large for dates baby 32.85 23.10 9 9255 466 50595394
Fatigue 31.33 23.10 51 9213 707550 49888310
Dyspnoea 30.83 23.10 33 9231 547575 50048285
Musculoskeletal deformity 30.41 23.10 10 9254 968 50594892
Eosinophilia 30.22 23.10 26 9238 18626 50577234
Mental disability 29.54 23.10 6 9258 82 50595778
Thymus hypoplasia 29.42 23.10 5 9259 23 50595837
CSF HIV escape syndrome 28.77 23.10 6 9258 94 50595766
Mitochondrial cytopathy 28.69 23.10 7 9257 228 50595632
Nephropathy toxic 28.58 23.10 18 9246 8011 50587849
Microcephaly 28.04 23.10 9 9255 807 50595053
Bacillus infection 27.58 23.10 8 9256 510 50595350
Bronchopulmonary dysplasia 27.42 23.10 7 9257 275 50595585
Diastasis recti abdominis 27.40 23.10 5 9259 37 50595823
Cholestasis 26.95 23.10 28 9236 25373 50570487
Small for dates baby 26.76 23.10 13 9251 3492 50592368
Antiviral drug level below therapeutic 26.53 23.10 5 9259 45 50595815
Hepatic cytolysis 25.96 23.10 17 9247 8086 50587774
Rash maculo-papular 25.84 23.10 28 9236 26613 50569247
Bacterial vulvovaginitis 25.79 23.10 8 9256 642 50595218
Chronic papillomatous dermatitis 25.79 23.10 5 9259 53 50595807
Patent ductus arteriosus 25.70 23.10 13 9251 3807 50592053
Arthralgia 25.15 23.10 26 9238 438676 50157184
Amniotic cavity infection 24.91 23.10 9 9255 1154 50594706
Dermatitis exfoliative 24.74 23.10 14 9250 5128 50590732
Abdominal discomfort 24.74 23.10 6 9258 231635 50364225
Heart disease congenital 24.45 23.10 9 9255 1217 50594643
Acute stress disorder 24.09 23.10 6 9258 213 50595647
Drug hypersensitivity 24.04 23.10 8 9256 251002 50344858
Hepatotoxicity 23.63 23.10 27 9237 27199 50568661

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 834.75 14.35 563 17591 84584 29471789
Drug interaction 803.93 14.35 779 17375 196606 29359767
Virologic failure 449.74 14.35 134 18020 2713 29553660
Lipodystrophy acquired 375.66 14.35 119 18035 2975 29553398
Immune reconstitution inflammatory syndrome 348.01 14.35 143 18011 7659 29548714
Foetal exposure during pregnancy 316.18 14.35 218 17936 33649 29522724
Pathogen resistance 302.71 14.35 131 18023 7985 29548388
Mitochondrial toxicity 260.98 14.35 85 18069 2326 29554047
Progressive external ophthalmoplegia 247.69 14.35 71 18083 1246 29555127
Viral mutation identified 230.48 14.35 78 18076 2410 29553963
Blood HIV RNA increased 218.82 14.35 61 18093 963 29555410
Eyelid ptosis 210.82 14.35 89 18065 5097 29551276
Loss of personal independence in daily activities 200.94 14.35 148 18006 25292 29531081
Viral load increased 142.87 14.35 52 18102 1997 29554376
Drug resistance 140.79 14.35 112 18042 21428 29534945
Psychiatric decompensation 115.50 14.35 41 18113 1463 29554910
Diplopia 109.72 14.35 80 18074 13438 29542935
Renal tubular disorder 105.11 14.35 52 18102 4300 29552073
CD4 lymphocytes decreased 98.33 14.35 37 18117 1561 29554812
Volvulus 94.08 14.35 33 18121 1136 29555237
Depression suicidal 94.02 14.35 34 18120 1281 29555092
Drug reaction with eosinophilia and systemic symptoms 79.70 14.35 92 18062 27900 29528473
Gene mutation 78.50 14.35 28 18126 1013 29555360
CSF HIV escape syndrome 78.30 14.35 19 18135 167 29556206
HIV-associated neurocognitive disorder 77.39 14.35 21 18133 298 29556075
Tearfulness 76.35 14.35 31 18123 1605 29554768
Brachydactyly 71.82 14.35 18 18136 183 29556190
Hepatitis C 70.64 14.35 52 18102 8858 29547515
Osteoporotic fracture 68.52 14.35 25 18129 966 29555407
Paranoia 59.51 14.35 49 18105 9828 29546545
Ophthalmoplegia 58.93 14.35 26 18128 1656 29554717
Depressive symptom 55.23 14.35 25 18129 1692 29554681
Hemivertebra 55.11 14.35 13 18141 100 29556273
Oesophageal atresia 52.49 14.35 17 18137 456 29555917
Genotype drug resistance test positive 49.86 14.35 20 18134 1003 29555370
Dyslipidaemia 49.46 14.35 36 18118 6025 29550348
Suicidal ideation 48.57 14.35 81 18073 34635 29521738
Cytomegalovirus chorioretinitis 48.07 14.35 28 18126 3210 29553163
Gastrointestinal tube insertion 47.95 14.35 20 18134 1109 29555264
Genital herpes 45.77 14.35 16 18138 545 29555828
Treatment failure 43.63 14.35 80 18074 36859 29519514
Osteoporosis 42.30 14.35 42 18112 10727 29545646
Drug level decreased 41.89 14.35 33 18121 6214 29550159
Oesophageal candidiasis 41.33 14.35 27 18127 3794 29552579
Renal impairment 40.73 14.35 126 18028 81207 29475166
Phalangeal hypoplasia 38.77 14.35 9 18145 64 29556309
Genital herpes simplex 38.47 14.35 10 18144 119 29556254
Anogenital dysplasia 38.24 14.35 10 18144 122 29556251
Premature baby 38.18 14.35 50 18104 17230 29539143
Laryngomalacia 37.81 14.35 12 18142 301 29556072
Anal cancer 36.03 14.35 12 18142 352 29556021
Dyspnoea 35.64 14.35 94 18060 326638 29229735
Blood creatine phosphokinase increased 34.80 14.35 77 18077 40567 29515806
Treatment noncompliance 34.51 14.35 57 18097 24170 29532203
Psychomotor skills impaired 34.27 14.35 21 18133 2640 29553733
Low birth weight baby 34.10 14.35 30 18124 6578 29549795
Completed suicide 33.98 14.35 7 18147 90239 29466134
Superior mesenteric artery syndrome 33.00 14.35 8 18146 70 29556303
Atrial fibrillation 32.68 14.35 12 18142 105634 29450739
Hypotension 32.58 14.35 43 18111 194311 29362062
Hepatic cirrhosis 32.22 14.35 42 18112 14402 29541971
Adverse event 31.86 14.35 43 18111 15248 29541125
Pneumonia 31.32 14.35 97 18057 320075 29236298
Drug abuse 30.48 14.35 6 18148 79877 29476496
Fanconi syndrome acquired 30.21 14.35 17 18137 1825 29554548
HIV lipodystrophy 29.83 14.35 6 18148 19 29556354
Congenital mitral valve incompetence 29.78 14.35 8 18146 109 29556264
Intestinal malrotation 28.74 14.35 6 18148 24 29556349
Congenital skin dimples 26.68 14.35 8 18146 165 29556208
HIV associated nephropathy 26.25 14.35 9 18145 289 29556084
Laryngectomy 25.59 14.35 4 18150 0 29556373
Dysphagia 25.56 14.35 83 18071 54843 29501530
Haemophilic arthropathy 25.43 14.35 7 18147 105 29556268
Syphilis 24.93 14.35 9 18145 337 29556036
Congenital vesicoureteric reflux 24.59 14.35 5 18149 17 29556356
Enanthema 24.56 14.35 9 18145 352 29556021
Strongyloidiasis 24.19 14.35 16 18138 2296 29554077
Fall 24.16 14.35 45 18109 177133 29379240
Hyperlipidaemia 24.12 14.35 34 18120 12556 29543817
Erosive duodenitis 24.01 14.35 13 18141 1294 29555079
Psychotic disorder 23.92 14.35 44 18110 20310 29536063
Osteonecrosis 23.69 14.35 35 18119 13484 29542889
Congenital foot malformation 23.64 14.35 9 18145 392 29555981
Nephropathy toxic 23.56 14.35 31 18123 10725 29545648
VACTERL syndrome 23.35 14.35 4 18150 3 29556370
Liver disorder 23.10 14.35 52 18102 27697 29528676
Cholestasis 23.02 14.35 47 18107 23415 29532958
Disease progression 22.61 14.35 11 18143 81905 29474468
Drug level increased 22.56 14.35 41 18113 18746 29537627
Hyperbilirubinaemia 22.43 14.35 36 18118 14898 29541475
HIV infection 22.41 14.35 12 18142 1169 29555204
Drug-induced liver injury 21.99 14.35 44 18110 21611 29534762
Antiviral drug level above therapeutic 21.61 14.35 5 18149 35 29556338
Acute hepatitis C 21.44 14.35 6 18148 96 29556277
Chronic hepatitis C 21.27 14.35 8 18146 337 29556036
Back pain 21.13 14.35 19 18135 102265 29454108
Lipohypertrophy 20.84 14.35 7 18147 211 29556162
Confusional state 20.69 14.35 29 18125 127848 29428525
Hemiparaesthesia 20.60 14.35 5 18149 44 29556329
Nephrolithiasis 20.56 14.35 47 18107 25287 29531086
Malignant neoplasm progression 20.26 14.35 10 18144 73849 29482524
Infection 20.15 14.35 11 18143 76740 29479633
Respiratory failure 20.11 14.35 18 18136 97113 29459260
Hepatic enzyme decreased 20.02 14.35 5 18149 50 29556323
Heart transplant rejection 19.91 14.35 11 18143 1140 29555233
Mycobacterium avium complex infection 19.71 14.35 14 18140 2255 29554118
Lymphoma 19.51 14.35 27 18127 9801 29546572
White matter lesion 19.45 14.35 9 18145 641 29555732
Glucose tolerance impaired 19.25 14.35 15 18139 2779 29553594
Hyperphagia 19.14 14.35 11 18143 1229 29555144
Jaundice 19.14 14.35 50 18104 29246 29527127
Acquired gene mutation 19.00 14.35 11 18143 1247 29555126
Atypical mycobacterial infection 18.80 14.35 9 18145 692 29555681
Congenital renal disorder 18.69 14.35 5 18149 67 29556306
Hypertriglyceridaemia 18.67 14.35 23 18131 7452 29548921
Choroiditis 18.64 14.35 10 18144 978 29555395
Hepatitis cholestatic 18.51 14.35 22 18132 6871 29549502
Drug ineffective 18.46 14.35 139 18015 363031 29193342
Constipation 18.35 14.35 26 18128 114134 29442239
Meningomyelocele 18.28 14.35 6 18148 168 29556205
Drug hypersensitivity 17.67 14.35 10 18144 68396 29487977
Nephrocalcinosis 17.65 14.35 8 18146 543 29555830
Febrile neutropenia 17.61 14.35 26 18128 112214 29444159
Cardiac arrest 17.55 14.35 16 18138 85575 29470798
Prescribed overdose 17.45 14.35 24 18130 8659 29547714
Infusion related reaction 17.37 14.35 3 18151 43883 29512490
Hepatitis 17.36 14.35 39 18115 20744 29535629
Cerebral ventricle dilatation 17.15 14.35 9 18145 841 29555532
Vertigo 17.13 14.35 40 18114 21821 29534552
Glycosuria 17.12 14.35 10 18144 1152 29555221
Congenital syphilis 17.11 14.35 3 18151 3 29556370
Tracheal fistula repair 17.11 14.35 3 18151 3 29556370
Cardiomyopathy acute 17.04 14.35 4 18150 30 29556343
Lymphocytic infiltration 16.93 14.35 8 18146 597 29555776
Maternal drugs affecting foetus 16.82 14.35 16 18138 3877 29552496
Myelocytosis 16.82 14.35 4 18150 32 29556341
Abnormal dreams 16.82 14.35 21 18133 6899 29549474
Congenital cystic kidney disease 16.75 14.35 7 18147 390 29555983
Myopathy 16.66 14.35 26 18128 10507 29545866
Toxicity to various agents 16.64 14.35 53 18101 173608 29382765
Retinal toxicity 16.63 14.35 7 18147 397 29555976
Renal failure 16.55 14.35 127 18027 118472 29437901
Immune reconstitution inflammatory syndrome associated tuberculosis 16.52 14.35 7 18147 404 29555969
Oesophageal carcinoma 16.51 14.35 17 18137 4530 29551843
Intensive care unit acquired weakness 16.28 14.35 9 18145 934 29555439
Blood pressure increased 16.10 14.35 13 18141 73790 29482583
Hepatic failure 15.91 14.35 49 18105 31463 29524910
Oxygen saturation decreased 15.88 14.35 4 18150 44933 29511440
Congenital hydronephrosis 15.79 14.35 8 18146 695 29555678
Kidney enlargement 15.75 14.35 8 18146 699 29555674
Birth trauma 15.58 14.35 3 18151 7 29556366
Pulmonary tuberculosis 15.43 14.35 16 18138 4299 29552074
Pancreatitis acute 15.30 14.35 41 18113 24344 29532029
Retinitis pigmentosa 15.28 14.35 4 18150 49 29556324
Pain 15.28 14.35 54 18100 171378 29384995
Cardio-respiratory arrest 15.21 14.35 6 18148 50595 29505778
Renal disorder 15.21 14.35 39 18115 22556 29533817
Subacute combined cord degeneration 15.10 14.35 5 18149 144 29556229
Hepatorenal syndrome 15.07 14.35 12 18142 2294 29554079
Seborrhoeic dermatitis 15.06 14.35 10 18144 1443 29554930
Tracheal deviation 15.04 14.35 3 18151 9 29556364
Liver transplant 15.02 14.35 12 18142 2304 29554069
Cachexia 15.00 14.35 19 18135 6330 29550043
Dermatitis exfoliative 14.82 14.35 19 18135 6406 29549967
Adrenal suppression 14.78 14.35 7 18147 525 29555848
Sepsis 14.77 14.35 42 18112 142640 29413733
Congenital ureteric anomaly 14.72 14.35 4 18150 57 29556316
Adrenogenital syndrome 14.66 14.35 4 18150 58 29556315
Hepatocellular injury 14.64 14.35 37 18117 21206 29535167
Chest discomfort 14.59 14.35 5 18149 45978 29510395

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
Virologic failure 876.88 14.60 208 21029 3258 64474237
Drug interaction 719.11 14.60 729 20508 361354 64116141
Depression 552.84 14.60 467 20770 182824 64294671
Pathogen resistance 542.41 14.60 190 21047 12353 64465142
Viral mutation identified 486.91 14.60 129 21108 3217 64474278
Immune reconstitution inflammatory syndrome 478.95 14.60 173 21064 12297 64465198
Lipodystrophy acquired 477.02 14.60 132 21105 3895 64473600
Blood HIV RNA increased 464.99 14.60 106 21131 1378 64476117
Mitochondrial toxicity 303.50 14.60 85 21152 2621 64474874
Progressive external ophthalmoplegia 296.09 14.60 72 21165 1255 64476240
Exposure during pregnancy 250.11 14.60 206 21031 77469 64400026
Viral load increased 237.87 14.60 69 21168 2418 64475077
Drug resistance 216.16 14.60 138 21099 34964 64442531
Eyelid ptosis 202.07 14.60 86 21151 9439 64468056
Abortion spontaneous 201.43 14.60 117 21120 25026 64452469
Maternal exposure during pregnancy 195.92 14.60 197 21040 95687 64381808
Drug reaction with eosinophilia and systemic symptoms 185.41 14.60 149 21088 54068 64423427
Loss of personal independence in daily activities 142.70 14.60 146 21091 72308 64405187
Psychiatric decompensation 128.59 14.60 43 21194 2420 64475075
Foetal exposure during pregnancy 117.25 14.60 47 21190 4429 64473066
Diplopia 112.08 14.60 83 21154 26682 64450813
CSF HIV escape syndrome 111.46 14.60 25 21212 300 64477195
Renal tubular disorder 107.26 14.60 48 21189 5939 64471556
CD4 lymphocytes decreased 105.61 14.60 37 21200 2398 64475097
Gene mutation 99.45 14.60 34 21203 2048 64475447
Depression suicidal 93.70 14.60 34 21203 2441 64475054
Treatment noncompliance 86.24 14.60 88 21149 43394 64434101
HIV-associated neurocognitive disorder 84.67 14.60 20 21217 306 64477189
Premature labour 84.58 14.60 44 21193 7576 64469919
Hepatitis C 82.25 14.60 49 21188 10966 64466529
Premature delivery 78.61 14.60 58 21179 18531 64458964
Abortion induced 71.23 14.60 37 21200 6351 64471144
Genotype drug resistance test positive 69.85 14.60 22 21215 1022 64476473
Tearfulness 69.73 14.60 33 21204 4640 64472855
Hyperbilirubinaemia 69.73 14.60 57 21180 21148 64456347
Renal impairment 66.43 14.60 141 21096 134876 64342619
Paranoia 64.64 14.60 49 21188 16303 64461192
Immune reconstitution inflammatory syndrome associated tuberculosis 63.21 14.60 19 21218 754 64476741
Caesarean section 61.23 14.60 41 21196 11233 64466262
Nephropathy toxic 59.53 14.60 48 21189 17466 64460029
Ophthalmoplegia 59.30 14.60 25 21212 2677 64474818
Live birth 59.06 14.60 40 21197 11164 64466331
Oesophageal candidiasis 58.13 14.60 35 21202 7982 64469513
Depressive symptom 55.82 14.60 28 21209 4468 64473027
Osteoporotic fracture 55.50 14.60 26 21211 3572 64473923
Premature baby 54.70 14.60 25 21212 3247 64474248
Foetal death 53.93 14.60 30 21207 5900 64471595
Dyslipidaemia 53.55 14.60 35 21202 9207 64468288
Genital herpes 53.47 14.60 21 21216 1874 64475621
Pain 51.61 14.60 64 21173 553447 63924048
Premature rupture of membranes 51.49 14.60 25 21212 3719 64473776
Hepatocellular injury 50.22 14.60 68 21169 45167 64432328
Completed suicide 48.21 14.60 8 21229 224406 64253089
Cytomegalovirus chorioretinitis 47.84 14.60 26 21211 4886 64472609
Renal failure 46.07 14.60 148 21089 181540 64295955
Psychomotor skills impaired 44.97 14.60 23 21214 3822 64473673
Fall 44.55 14.60 43 21194 416783 64060712
Drug-induced liver injury 43.15 14.60 65 21172 47578 64429917
Hepatic cirrhosis 42.90 14.60 48 21189 26250 64451245
Dyspnoea 42.75 14.60 110 21127 718564 63758931
Fanconi syndrome acquired 42.06 14.60 19 21218 2402 64475093
Peripheral swelling 41.64 14.60 9 21228 209144 64268351
Drug hypersensitivity 40.30 14.60 14 21223 237801 64239694
Syphilis 40.17 14.60 12 21225 466 64477029
Generalised anxiety disorder 39.64 14.60 17 21220 1898 64475597
Joint swelling 39.50 14.60 11 21226 215371 64262124
Cholestasis 38.91 14.60 60 21177 44812 64432683
Pulmonary tuberculosis 38.51 14.60 26 21211 7218 64470277
Mitochondrial cytopathy 38.00 14.60 11 21226 382 64477113
Stillbirth 37.54 14.60 20 21217 3613 64473882
Dermatitis exfoliative 36.51 14.60 29 21208 10323 64467172
Genital herpes simplex 35.92 14.60 10 21227 301 64477194
Suicidal ideation 35.63 14.60 72 21165 66470 64411025
Cachexia 35.06 14.60 27 21210 9190 64468305
HIV lipodystrophy 34.60 14.60 6 21231 15 64477480
Spina bifida 34.00 14.60 7 21230 54 64477441
Mycoplasma genitalium infection 33.80 14.60 6 21231 18 64477477
Blood creatine phosphokinase increased 33.32 14.60 65 21172 58493 64419002
Liver transplant 32.63 14.60 19 21218 4073 64473422
Strongyloidiasis 31.89 14.60 17 21220 3073 64474422
Superior mesenteric artery syndrome 31.80 14.60 8 21229 161 64477334
Renal tubular dysfunction 31.75 14.60 11 21226 689 64476806
HIV associated nephropathy 31.68 14.60 9 21228 292 64477203
Enanthema 31.14 14.60 11 21226 730 64476765
Psychotic disorder 31.05 14.60 47 21190 34531 64442964
Atrial fibrillation 30.88 14.60 9 21228 171080 64306415
Cushingoid 30.52 14.60 23 21214 7580 64469915
Central obesity 30.39 14.60 13 21224 1442 64476053
Anogenital dysplasia 29.95 14.60 7 21230 102 64477393
Infection 29.44 14.60 12 21225 184868 64292627
Drug ineffective 29.37 14.60 160 21077 840087 63637408
Abdominal discomfort 28.77 14.60 12 21225 182310 64295185
Erosive duodenitis 28.61 14.60 13 21224 1665 64475830
Hepatitis cholestatic 28.56 14.60 27 21210 12128 64465367
White matter lesion 28.29 14.60 13 21224 1709 64475786
Adrenal suppression 28.20 14.60 12 21225 1315 64476180
Nephrolithiasis 27.97 14.60 51 21186 43632 64433863
Jaundice 27.78 14.60 54 21183 48458 64429037
Rash maculo-papular 27.73 14.60 53 21184 46973 64430522
Pancreatitis acute 27.40 14.60 50 21187 42805 64434690
Hepatic failure 27.38 14.60 58 21179 55336 64422159
Hepatic cytolysis 27.05 14.60 28 21209 14021 64463474
Proteinuria 26.79 14.60 39 21198 27684 64449811
Back pain 26.47 14.60 26 21211 250145 64227350
Injection site pain 26.20 14.60 3 21234 111405 64366090
Drug intolerance 25.69 14.60 15 21222 187977 64289518
Mycobacterium avium complex infection 25.50 14.60 16 21221 3924 64473571
Pancytopenia 25.45 14.60 104 21133 143205 64334290
Hepatic encephalopathy 25.42 14.60 33 21204 21033 64456462
Hepatitis fulminant 25.23 14.60 19 21218 6255 64471240
Cholestasis of pregnancy 25.22 14.60 10 21227 915 64476580
Anal cancer 25.07 14.60 9 21228 626 64476869
Acute hepatitis C 25.07 14.60 7 21230 213 64477282
Acute stress disorder 24.93 14.60 8 21229 395 64477100
Retinal toxicity 24.90 14.60 11 21226 1319 64476176
Nephrocalcinosis 24.87 14.60 11 21226 1323 64476172
HIV infection 24.64 14.60 10 21227 972 64476523
Confusional state 24.47 14.60 30 21207 261114 64216381
Antiviral drug level below therapeutic 24.12 14.60 5 21232 40 64477455
Haemolytic anaemia 23.98 14.60 28 21209 16025 64461470
Choroiditis 23.66 14.60 10 21227 1077 64476418
Hepatotoxicity 23.52 14.60 45 21192 39917 64437578
Pain in extremity 23.31 14.60 40 21197 303045 64174450
Pre-eclampsia 23.15 14.60 18 21219 6213 64471282
Chest discomfort 23.09 14.60 5 21232 116101 64361394
Brachydactyly 23.07 14.60 4 21233 10 64477485
Aspartate aminotransferase increased 22.93 14.60 89 21148 119699 64357796
Hypotension 22.81 14.60 58 21179 380916 64096579
Oesophageal carcinoma 22.80 14.60 16 21221 4727 64472768
Contraindicated product administered 22.79 14.60 4 21233 107825 64369670
Hypertriglyceridaemia 22.79 14.60 23 21214 11182 64466313
Face oedema 22.72 14.60 34 21203 24727 64452768
Oxygen saturation decreased 22.60 14.60 4 21233 107172 64370323
Eosinophilia 22.56 14.60 43 21194 38033 64439462
Multiple-drug resistance 22.47 14.60 18 21219 6484 64471011
Sinusitis 22.39 14.60 10 21227 145918 64331577
Nasopharyngitis 22.37 14.60 19 21218 196054 64281441
Drug level decreased 22.28 14.60 23 21214 11480 64466015
Abortion spontaneous incomplete 21.85 14.60 4 21233 15 64477480
Dysphagia 21.80 14.60 81 21156 106731 64370764
Product size issue 21.73 14.60 8 21229 598 64476897
Treatment failure 21.72 14.60 86 21151 116730 64360765
Hepatitis B 21.71 14.60 19 21218 7726 64469769
Tuberculosis 21.61 14.60 24 21213 13014 64464481
Therapeutic product effect decreased 20.93 14.60 6 21231 115345 64362150
Acquired gene mutation 20.71 14.60 11 21226 1975 64475520
Mycobacterium avium complex immune restoration disease 20.60 14.60 4 21233 22 64477473
Blood pressure increased 20.58 14.60 16 21221 172536 64304959
Hepatitis 20.55 14.60 46 21191 45536 64431959
Contusion 20.55 14.60 6 21231 113959 64363536
Viral load decreased 20.30 14.60 4 21233 24 64477471
Hepatic enzyme decreased 20.15 14.60 5 21232 95 64477400
Pneumocystis jirovecii pneumonia 19.93 14.60 34 21203 27600 64449895
Bacterial vulvovaginitis 19.82 14.60 7 21230 464 64477031
Lipohypertrophy 19.65 14.60 8 21229 784 64476711
Alanine aminotransferase increased 19.47 14.60 94 21143 138937 64338558
Psychomotor retardation 19.42 14.60 15 21222 5128 64472367
Pneumonia 19.24 14.60 107 21130 559469 63918026
Gastroschisis 18.98 14.60 3 21234 3 64477492
Renal colic 18.97 14.60 11 21226 2341 64475154
Hemiparaesthesia 18.96 14.60 5 21232 122 64477373
Lower respiratory tract infection 18.96 14.60 4 21233 94610 64382885
Chronic hepatitis C 18.85 14.60 7 21230 536 64476959
Osteoporosis 18.45 14.60 42 21195 42038 64435457
Toxic skin eruption 18.44 14.60 27 21210 19257 64458238
Chronic kidney disease 18.26 14.60 51 21186 57868 64419627
Stevens-Johnson syndrome 18.25 14.60 37 21200 34212 64443283
Constipation 17.87 14.60 30 21207 229307 64248188
Polyhydramnios 17.69 14.60 9 21228 1478 64476017
Therapeutic product effect incomplete 17.67 14.60 6 21231 103476 64374019
Lymphadenopathy 17.66 14.60 44 21193 46642 64430853
Glycosuria 17.53 14.60 10 21227 2064 64475431
Sudden infant death syndrome 17.49 14.60 5 21232 166 64477329
Prescribed overdose 17.36 14.60 27 21210 20304 64457191
Blood creatinine increased 17.03 14.60 89 21148 135693 64341802
Anaemia 17.01 14.60 195 21042 378485 64099010
Plasmablastic lymphoma 16.92 14.60 6 21231 403 64477092
Osteonecrosis 16.87 14.60 32 21205 28197 64449298
Bacillus infection 16.70 14.60 7 21230 739 64476756
Alopecia 16.63 14.60 18 21219 165672 64311823
Musculoskeletal stiffness 16.59 14.60 10 21227 123196 64354299
Intensive care unit acquired weakness 16.43 14.60 9 21228 1718 64475777
Lactic acidosis 16.43 14.60 51 21186 61359 64416136
Foetal growth restriction 16.41 14.60 9 21228 1721 64475774
Heart rate increased 16.37 14.60 6 21231 98669 64378826
Loss of consciousness 16.17 14.60 15 21222 148350 64329145
Seborrhoeic dermatitis 15.96 14.60 9 21228 1817 64475678
Urticaria 15.93 14.60 15 21222 147302 64330193
HIV viraemia 15.93 14.60 4 21233 80 64477415
Hepatic function abnormal 15.91 14.60 52 21185 64261 64413234
Atypical mycobacterial infection 15.81 14.60 8 21229 1300 64476195
Underweight 15.65 14.60 7 21230 864 64476631
Hyperhidrosis 15.65 14.60 11 21226 124909 64352586
Glomerulonephritis membranous 15.62 14.60 8 21229 1332 64476163
Fat tissue decreased 15.61 14.60 4 21233 87 64477408
Arthralgia 15.49 14.60 84 21153 442176 64035319
Asthma 15.45 14.60 6 21231 95219 64382276
Congestive cardiomyopathy 15.38 14.60 18 21219 10326 64467169
Lymphocytic infiltration 15.27 14.60 8 21229 1396 64476099
Progressive multifocal leukoencephalopathy 15.27 14.60 24 21213 18208 64459287
Giardiasis 15.24 14.60 5 21232 265 64477230
Acute haemorrhagic conjunctivitis 15.23 14.60 3 21234 18 64477477
Plagiocephaly 15.23 14.60 3 21234 18 64477477
Feeling abnormal 15.17 14.60 13 21224 133589 64343906
Hyperlipidaemia 14.93 14.60 27 21210 22949 64454546
Mitochondrial myopathy 14.90 14.60 5 21232 284 64477211
Anal cancer stage 0 14.70 14.60 3 21234 22 64477473
Hepatitis acute 14.66 14.60 20 21217 13369 64464126

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AJ01 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Integrase inhibitors
ATC J05AR16 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
FDA MoA N0000000127 HIV Integrase 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 D019428 HIV Integrase Inhibitors
MeSH PA D019429 Integrase Inhibitors
FDA EPC N0000175887 Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor
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
Disorder of muscle contraindication 129565002 DOID:423
Rhabdomyolysis contraindication 240131006
Breastfeeding (mother) contraindication 413712001




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 8.19 acidic
pKa2 10.89 acidic
pKa3 12.18 acidic
pKa4 2.3 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 400MG BASE ISENTRESS MERCK SHARP DOHME N022145 Oct. 12, 2007 RX TABLET ORAL 7217713 Oct. 21, 2022 TREATMENT OF HIV INFECTION
EQ 400MG BASE ISENTRESS MERCK SHARP DOHME N022145 Oct. 12, 2007 RX TABLET ORAL 7435734 Oct. 21, 2022 INTEGRASE INHIBITION FOR THE TREATMENT OF HIV INFECTION
EQ 400MG BASE ISENTRESS MERCK SHARP DOHME N022145 Oct. 12, 2007 RX TABLET ORAL 7435734 Oct. 21, 2022 TREATMENT OF HIV INFECTION
EQ 600MG BASE ISENTRESS HD MERCK SHARP DOHME N022145 May 26, 2017 RX TABLET ORAL 7217713 Oct. 21, 2022 TREATMENT OF HIV INFECTION
EQ 600MG BASE ISENTRESS HD MERCK SHARP DOHME N022145 May 26, 2017 RX TABLET ORAL 7435734 Oct. 21, 2022 INTEGRASE INHIBITION FOR THE TREATMENT OF HIV INFECTION
EQ 600MG BASE ISENTRESS HD MERCK SHARP DOHME N022145 May 26, 2017 RX TABLET ORAL 7435734 Oct. 21, 2022 TREATMENT OF HIV INFECTION
EQ 100MG BASE ISENTRESS MERCK SHARP DOHME N203045 Dec. 21, 2011 RX TABLET, CHEWABLE ORAL 7217713 Oct. 21, 2022 TREATMENT OF HIV INFECTION
EQ 100MG BASE ISENTRESS MERCK SHARP DOHME N203045 Dec. 21, 2011 RX TABLET, CHEWABLE ORAL 7435734 Oct. 21, 2022 TREATMENT OF HIV INFECTION
EQ 25MG BASE ISENTRESS MERCK SHARP DOHME N203045 Dec. 21, 2011 RX TABLET, CHEWABLE ORAL 7217713 Oct. 21, 2022 TREATMENT OF HIV INFECTION
EQ 25MG BASE ISENTRESS MERCK SHARP DOHME N203045 Dec. 21, 2011 RX TABLET, CHEWABLE ORAL 7435734 Oct. 21, 2022 TREATMENT OF HIV INFECTION
EQ 100MG BASE/PACKET ISENTRESS MERCK SHARP DOHME N205786 Dec. 20, 2013 RX POWDER ORAL 7217713 Oct. 21, 2022 TREATMENT OF HIV INFECTION
EQ 100MG BASE/PACKET ISENTRESS MERCK SHARP DOHME N205786 Dec. 20, 2013 RX POWDER ORAL 7435734 Oct. 21, 2022 TREATMENT OF HIV INFECTION
150MG;EQ 300MG BASE DUTREBIS MERCK SHARP DOHME N206510 Feb. 6, 2015 DISCN TABLET ORAL 7217713 Oct. 21, 2022 TREATMENT OF HIV-1 INFECTION
150MG;EQ 300MG BASE DUTREBIS MERCK SHARP DOHME N206510 Feb. 6, 2015 DISCN TABLET ORAL 7435734 Oct. 21, 2022 TREATMENT OF HIV-1 INFECTION
EQ 400MG BASE ISENTRESS MERCK SHARP DOHME N022145 Oct. 12, 2007 RX TABLET ORAL 7754731 March 11, 2029 TREATMENT OF HIV INFECTION
EQ 600MG BASE ISENTRESS HD MERCK SHARP DOHME N022145 May 26, 2017 RX TABLET ORAL 7754731 March 11, 2029 TREATMENT OF HIV INFECTION
EQ 100MG BASE ISENTRESS MERCK SHARP DOHME N203045 Dec. 21, 2011 RX TABLET, CHEWABLE ORAL 7754731 March 11, 2029 TREATMENT OF HIV INFECTION
EQ 25MG BASE ISENTRESS MERCK SHARP DOHME N203045 Dec. 21, 2011 RX TABLET, CHEWABLE ORAL 7754731 March 11, 2029 TREATMENT OF HIV INFECTION
EQ 100MG BASE/PACKET ISENTRESS MERCK SHARP DOHME N205786 Dec. 20, 2013 RX POWDER ORAL 7754731 March 11, 2029 TREATMENT OF HIV INFECTION
150MG;EQ 300MG BASE DUTREBIS MERCK SHARP DOHME N206510 Feb. 6, 2015 DISCN TABLET ORAL 7754731 March 11, 2029 TREATMENT OF HIV-1 INFECTION
EQ 600MG BASE ISENTRESS HD MERCK SHARP DOHME N022145 May 26, 2017 RX TABLET ORAL 10772888 March 30, 2032 TREATMENT OF HIV-1 INFECTION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
C-C chemokine receptor type 1 GPCR Ki 8.30 CHEMBL
Integrase Enzyme INHIBITOR IC50 8 CHEMBL CHEMBL
Gag-Pol polyprotein Polyprotein INHIBITOR IC50 7.52 WOMBAT-PK
Integrase Enzyme IC50 5.74 CHEMBL

External reference:

IDSource
D06676 KEGG_DRUG
871038-72-1 SECONDARY_CAS_RN
4026736 VANDF
C1966407 UMLSCUI
CHEBI:82960 CHEBI
RLT PDB_CHEM_ID
CHEMBL254316 ChEMBL_ID
CHEMBL518520 ChEMBL_ID
D000068898 MESH_DESCRIPTOR_UI
DB06817 DRUGBANK_ID
11571 IUPHAR_LIGAND_ID
8842 INN_ID
22VKV8053U UNII
54671008 PUBCHEM_CID
1235585 RXNORM
121359 MMSL
24597 MMSL
31069 MMSL
d07048 MMSL
012364 NDDF
012365 NDDF
1149432009 SNOMEDCT_US
429368003 SNOMEDCT_US
429707008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 0006-0227 TABLET, FILM COATED 400 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 0006-0227 TABLET, FILM COATED 400 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 0006-0473 TABLET, CHEWABLE 25 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 0006-0473 TABLET, CHEWABLE 25 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 0006-0477 TABLET, CHEWABLE 100 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 0006-0477 TABLET, CHEWABLE 100 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 0006-3080 TABLET, FILM COATED 600 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 0006-3080 TABLET, FILM COATED 600 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 0006-3603 GRANULE, FOR SUSPENSION 100 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 0006-3603 GRANULE, FOR SUSPENSION 100 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 50090-1085 TABLET, FILM COATED 400 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 53808-0650 TABLET, FILM COATED 400 mg ORAL NDA 28 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 54868-0117 TABLET, FILM COATED 400 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 61919-706 TABLET, FILM COATED 400 mg ORAL NDA 17 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 61919-706 TABLET, FILM COATED 400 mg ORAL NDA 17 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 66336-214 TABLET, FILM COATED 400 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 67296-1235 TABLET, FILM COATED 400 mg ORAL NDA 18 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 68071-2113 TABLET, FILM COATED 400 mg ORAL NDA 29 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 70518-1621 TABLET, FILM COATED 400 mg ORAL NDA 30 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 76519-1130 TABLET, FILM COATED 400 mg ORAL NDA 17 sections