raltegravir 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: 1.16
  • 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 ┬ÁM/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 1159.48 22.13 518 8776 124342 53215430
Foetal exposure during pregnancy 529.02 22.13 206 9088 34509 53305263
Maternal exposure during pregnancy 308.52 22.13 238 9056 155401 53184371
Abortion spontaneous 247.77 22.13 133 9161 46502 53293270
Virologic failure 227.05 22.13 57 9237 2207 53337565
Premature baby 207.40 22.13 90 9204 19711 53320061
Immune reconstitution inflammatory syndrome 180.93 22.13 60 9234 6286 53333486
Drug reaction with eosinophilia and systemic symptoms 126.65 22.13 76 9218 32724 53307048
Pathogen resistance 125.23 22.13 46 9248 6514 53333258
Lipodystrophy acquired 123.87 22.13 33 9261 1617 53338155
Blood HIV RNA increased 115.21 22.13 27 9267 778 53338994
Viral load increased 113.11 22.13 30 9264 1445 53338327
Premature labour 112.68 22.13 51 9243 12311 53327461
Premature delivery 112.63 22.13 65 9229 26039 53313733
Caesarean section 104.93 22.13 54 9240 17266 53322506
Viral mutation identified 102.99 22.13 30 9264 2044 53337728
Ectopic kidney 91.82 22.13 16 9278 93 53339679
Live birth 91.36 22.13 47 9247 15012 53324760
Abortion induced 87.21 22.13 41 9253 10785 53328987
Treatment noncompliance 86.57 22.13 60 9234 32975 53306797
Foetal growth restriction 86.29 22.13 36 9258 7138 53332634
Sudden infant death syndrome 85.33 22.13 17 9277 221 53339551
Spina bifida 79.99 22.13 20 9274 760 53339012
Drug resistance 78.96 22.13 47 9247 19915 53319857
Cloacal exstrophy 72.51 22.13 14 9280 153 53339619
Foetal death 71.00 22.13 34 9260 9313 53330459
Congenital genital malformation 67.42 22.13 13 9281 141 53339631
Bladder agenesis 67.00 22.13 13 9281 146 53339626
Congenital heart valve disorder 66.45 22.13 12 9282 88 53339684
Genitalia external ambiguous 65.91 22.13 13 9281 160 53339612
Neonatal respiratory arrest 64.19 22.13 11 9283 57 53339715
Meconium stain 63.84 22.13 13 9281 190 53339582
Premature rupture of membranes 63.51 22.13 26 9268 4914 53334858
Gastrointestinal disorder congenital 63.03 22.13 12 9282 121 53339651
Hepatocellular injury 61.57 22.13 47 9247 29939 53309833
Tethered cord syndrome 61.29 22.13 13 9281 234 53339538
Meningomyelocele 60.27 22.13 15 9279 559 53339213
Gastroschisis 60.24 22.13 13 9281 255 53339517
Anal atresia 59.71 22.13 14 9280 404 53339368
Caudal regression syndrome 59.67 22.13 12 9282 164 53339608
Congenital pulmonary valve disorder 57.55 22.13 10 9284 57 53339715
Hemivertebra 56.99 22.13 11 9283 120 53339652
Complication of delivery 54.59 22.13 11 9283 152 53339620
Immune reconstitution inflammatory syndrome associated tuberculosis 54.48 22.13 13 9281 405 53339367
Gastrointestinal malformation 53.26 22.13 11 9283 173 53339599
Spine malformation 52.60 22.13 12 9282 306 53339466
Maternal drugs affecting foetus 50.90 22.13 23 9271 5523 53334249
Exomphalos 50.50 22.13 13 9281 556 53339216
Umbilical cord abnormality 48.74 22.13 13 9281 639 53339133
CD4 lymphocytes decreased 48.13 22.13 16 9278 1685 53338087
Pulmonary valve sclerosis 47.09 22.13 8 9286 39 53339733
Congenital choroid plexus cyst 46.37 22.13 11 9283 334 53339438
Generalised anxiety disorder 45.59 22.13 16 9278 1984 53337788
Pain 45.48 22.13 23 9271 588375 52751397
Congenital anomaly 44.92 22.13 15 9279 1602 53338170
Cardiac murmur 44.38 22.13 27 9267 11886 53327886
Hyperbilirubinaemia 43.60 22.13 26 9268 11043 53328729
Stillbirth 43.49 22.13 22 9272 6775 53332997
Drug interaction 42.69 22.13 108 9186 219221 53120551
Cholestasis of pregnancy 40.81 22.13 13 9281 1196 53338576
Fall 40.29 22.13 7 9287 358433 52981339
Renal tubular dysfunction 39.79 22.13 10 9284 388 53339384
Drug ineffective 39.47 22.13 51 9243 817194 52522578
Low birth weight baby 39.06 22.13 20 9274 6317 53333455
Pre-eclampsia 38.52 22.13 22 9272 8625 53331147
Gestational diabetes 37.28 22.13 21 9273 8018 53331754
Hepatitis fulminant 36.39 22.13 16 9278 3603 53336169
Genotype drug resistance test positive 35.99 22.13 10 9284 574 53339198
Congenital ectopic bladder 35.21 22.13 7 9287 90 53339682
Neural tube defect 34.42 22.13 8 9286 222 53339550
Viral load decreased 34.41 22.13 6 9288 35 53339737
Product size issue 34.03 22.13 9 9285 428 53339344
Anencephaly 33.95 22.13 8 9286 236 53339536
Oesophageal candidiasis 32.98 22.13 17 9277 5443 53334329
Ventricular hypertrophy 32.61 22.13 15 9279 3750 53336022
Large for dates baby 32.50 22.13 9 9285 510 53339262
Hydrocephalus 30.76 22.13 16 9278 5220 53334552
Central obesity 30.13 22.13 10 9284 1048 53338724
Congenital hydrocephalus 30.12 22.13 7 9287 194 53339578
Fatigue 29.94 22.13 51 9243 730455 52609317
Anaemia 29.16 22.13 110 9184 276608 53063164
Thymus hypoplasia 29.16 22.13 5 9289 26 53339746
Congenital musculoskeletal anomaly 28.40 22.13 8 9286 483 53339289
Microcephaly 28.34 22.13 9 9285 820 53338952
Eosinophilia 28.32 22.13 26 9268 21309 53318463
Nephropathy toxic 28.32 22.13 18 9276 8554 53331218
CSF HIV escape syndrome 28.23 22.13 6 9288 109 53339663
Mental disability 27.88 22.13 6 9288 116 53339656
Bronchopulmonary dysplasia 27.15 22.13 7 9287 301 53339471
Dyspnoea 26.78 22.13 38 9256 586194 52753578
Diastasis recti abdominis 26.77 22.13 5 9289 45 53339727
Small for dates baby 26.53 22.13 13 9281 3739 53336033
Mitochondrial cytopathy 26.45 22.13 7 9287 334 53339438
Rash maculo-papular 26.15 22.13 29 9265 29720 53310052
Antiviral drug level below therapeutic 25.95 22.13 5 9289 54 53339718
Chronic papillomatous dermatitis 25.46 22.13 5 9289 60 53339712
Patent ductus arteriosus 25.39 22.13 13 9281 4105 53335667
Cholestasis 25.27 22.13 28 9266 28667 53311105
Hepatic cytolysis 24.67 22.13 16 9278 7869 53331903
Amniotic cavity infection 24.58 22.13 9 9285 1261 53338511
Heart disease congenital 24.49 22.13 9 9285 1274 53338498
Hepatotoxicity 24.20 22.13 27 9267 27853 53311919
Acute stress disorder 24.04 22.13 6 9288 226 53339546
Sepsis neonatal 23.98 22.13 7 9287 480 53339292
Dermatitis exfoliative 23.52 22.13 14 9280 5922 53333850
Pulmonary tuberculosis 23.31 22.13 13 9281 4868 53334904
Musculoskeletal deformity 23.10 22.13 8 9286 953 53338819
Alanine aminotransferase increased 22.98 22.13 51 9243 95044 53244728
Aqueductal stenosis 22.84 22.13 4 9290 24 53339748
Hemiataxia 22.84 22.13 4 9290 24 53339748
Bacillus infection 22.83 22.13 7 9287 568 53339204
HIV infection 22.63 22.13 7 9287 585 53339187
Drug hypersensitivity 22.56 22.13 9 9285 265233 53074539

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 726.82 14.59 525 17657 96535 32398809
Drug interaction 704.64 14.59 728 17454 217457 32277887
Virologic failure 395.47 14.59 127 18055 3660 32491684
Immune reconstitution inflammatory syndrome 359.43 14.59 151 18031 9408 32485936
Lipodystrophy acquired 350.02 14.59 115 18067 3567 32491777
Foetal exposure during pregnancy 279.85 14.59 211 17971 41090 32454254
Pathogen resistance 265.91 14.59 122 18060 9388 32485956
Mitochondrial toxicity 249.37 14.59 82 18100 2548 32492796
Progressive external ophthalmoplegia 236.02 14.59 67 18115 1251 32494093
Viral mutation identified 203.80 14.59 73 18109 2946 32492398
Eyelid ptosis 199.76 14.59 85 18097 5457 32489887
Blood HIV RNA increased 167.82 14.59 54 18128 1563 32493781
Loss of personal independence in daily activities 161.74 14.59 128 18054 26705 32468639
Drug resistance 143.68 14.59 112 18070 22853 32472491
Viral load increased 139.56 14.59 56 18126 3094 32492250
Diplopia 102.25 14.59 76 18106 14436 32480908
Renal tubular disorder 100.91 14.59 52 18130 5150 32490194
Gene mutation 82.54 14.59 28 18154 958 32494386
Depression suicidal 80.14 14.59 30 18152 1372 32493972
Volvulus 77.58 14.59 29 18153 1321 32494023
Drug reaction with eosinophilia and systemic symptoms 77.19 14.59 93 18089 32392 32462952
Psychiatric decompensation 74.50 14.59 29 18153 1477 32493867
Brachydactyly 74.22 14.59 18 18164 175 32495169
CD4 lymphocytes decreased 73.67 14.59 32 18150 2158 32493186
HIV infection 70.91 14.59 30 18152 1896 32493448
Extraocular muscle paresis 68.32 14.59 21 18161 521 32494823
Osteoporotic fracture 66.38 14.59 25 18157 1163 32494181
CSF HIV escape syndrome 65.84 14.59 16 18166 157 32495187
Ophthalmoplegia 64.97 14.59 26 18156 1425 32493919
Tearfulness 64.23 14.59 27 18155 1679 32493665
Hepatitis C 61.77 14.59 55 18127 13463 32481881
HIV-associated neurocognitive disorder 57.11 14.59 17 18165 377 32494967
Paranoia 51.46 14.59 45 18137 10754 32484590
Cytomegalovirus chorioretinitis 47.66 14.59 28 18154 3584 32491760
Oesophageal candidiasis 47.42 14.59 30 18152 4384 32490960
Treatment failure 46.94 14.59 81 18101 39082 32456262
Dyslipidaemia 46.14 14.59 35 18147 6848 32488496
Genital herpes 45.79 14.59 16 18166 599 32494745
Gastrointestinal tube insertion 45.58 14.59 20 18162 1382 32493962
Hemivertebra 45.53 14.59 11 18171 105 32495239
Oesophageal atresia 44.70 14.59 15 18167 496 32494848
Drug level decreased 43.70 14.59 33 18149 6413 32488931
Osteoporosis 43.07 14.59 43 18139 12139 32483205
Genotype drug resistance test positive 41.00 14.59 20 18162 1761 32493583
Depressive symptom 40.20 14.59 20 18162 1838 32493506
Genital herpes simplex 38.51 14.59 10 18172 131 32495213
Laryngomalacia 38.00 14.59 12 18170 326 32495018
Suicidal ideation 37.07 14.59 72 18110 38011 32457333
Renal impairment 36.70 14.59 124 18058 91848 32403496
Anogenital dysplasia 36.09 14.59 10 18172 170 32495174
Premature baby 36.01 14.59 48 18134 18470 32476874
Low birth weight baby 35.05 14.59 30 18152 6964 32488380
Atrial fibrillation 34.76 14.59 11 18171 116693 32378651
Anal cancer 34.45 14.59 12 18170 445 32494899
Superior mesenteric artery syndrome 33.54 14.59 8 18174 72 32495272
Dyspnoea 32.21 14.59 100 18082 361945 32133399
Blood creatine phosphokinase increased 31.61 14.59 75 18107 45401 32449943
Pneumonia 30.99 14.59 99 18083 355153 32140191
Completed suicide 30.79 14.59 7 18175 92510 32402834
HIV lipodystrophy 30.39 14.59 6 18176 19 32495325
Hepatic cirrhosis 30.30 14.59 42 18140 16767 32478577
Hypotension 29.62 14.59 47 18135 216063 32279281
Congenital mitral valve incompetence 29.44 14.59 8 18174 126 32495218
Fanconi syndrome acquired 28.67 14.59 17 18165 2213 32493131
Congenital skin dimples 27.56 14.59 8 18174 162 32495182
Psychomotor skills impaired 26.86 14.59 17 18165 2486 32492858
Drug abuse 26.84 14.59 6 18176 80237 32415107
Intestinal malrotation 26.74 14.59 6 18176 40 32495304
Adverse event 26.52 14.59 39 18143 16433 32478911
Spine malformation 25.42 14.59 8 18174 215 32495129
HIV associated nephropathy 25.00 14.59 9 18173 368 32494976
Confusional state 24.88 14.59 26 18156 143089 32352255
Dysphagia 24.60 14.59 83 18099 61393 32433951
Hyperlipidaemia 24.29 14.59 35 18147 14476 32480868
Enanthema 24.13 14.59 9 18173 407 32494937
Strongyloidiasis 24.05 14.59 16 18166 2545 32492799
Fall 23.84 14.59 46 18136 196155 32299189
Erosive duodenitis 23.70 14.59 13 18169 1459 32493885
Treatment noncompliance 23.56 14.59 49 18133 27153 32468191
Nephrolithiasis 23.37 14.59 49 18133 27305 32468039
Drug level increased 23.35 14.59 41 18141 20039 32475305
Nephropathy toxic 23.28 14.59 31 18151 11915 32483429
Congenital vesicoureteric reflux 23.18 14.59 5 18177 27 32495317
Haemophilic arthropathy 22.42 14.59 7 18175 183 32495161
Acquired immunodeficiency syndrome 22.42 14.59 9 18173 497 32494847
Mycobacterium avium complex infection 22.17 14.59 16 18166 2901 32492443
Osteonecrosis 22.06 14.59 36 18146 16586 32478758
Drug-induced liver injury 21.61 14.59 44 18138 24019 32471325
Cholestasis 21.46 14.59 47 18135 26986 32468358
Disease progression 21.28 14.59 11 18171 86851 32408493
Lymphoma 21.00 14.59 28 18154 10772 32484572
Laryngectomy 20.95 14.59 4 18178 10 32495334
Syphilis 20.90 14.59 9 18173 594 32494750
Hypertriglyceridaemia 20.75 14.59 25 18157 8694 32486650
Liver disorder 20.70 14.59 51 18131 31603 32463741
Back pain 20.65 14.59 19 18163 111034 32384310
Hyperbilirubinaemia 20.36 14.59 36 18146 17694 32477650
Respiratory failure 20.33 14.59 18 18164 107164 32388180
VACTERL syndrome 20.18 14.59 4 18178 13 32495331
Antiviral drug level above therapeutic 20.06 14.59 5 18177 55 32495289
Acquired gene mutation 20.04 14.59 11 18171 1236 32494108
Hemiparaesthesia 19.89 14.59 5 18177 57 32495287
Constipation 19.75 14.59 25 18157 126348 32368996
Heart transplant rejection 19.53 14.59 11 18171 1300 32494044
Oesophageal carcinoma 19.26 14.59 17 18165 4109 32491235
White matter lesion 19.21 14.59 9 18173 724 32494620
Jaundice 19.21 14.59 52 18130 34106 32461238
Malignant neoplasm progression 19.14 14.59 10 18172 78486 32416858
Infection 18.93 14.59 12 18170 84703 32410641
Chronic hepatitis C 18.93 14.59 8 18174 504 32494840
Hepatic enzyme decreased 18.75 14.59 5 18177 73 32495271
Lipohypertrophy 18.68 14.59 7 18175 321 32495023
Cardiac arrest 18.66 14.59 16 18166 96760 32398584
Hyperphagia 18.63 14.59 11 18171 1420 32493924
Hepatitis cholestatic 18.63 14.59 23 18159 8202 32487142
Hepatitis 18.59 14.59 41 18141 23652 32471692
Choroiditis 18.57 14.59 10 18172 1082 32494262
Congenital renal disorder 18.51 14.59 5 18177 77 32495267
Myopathy 18.47 14.59 27 18155 11314 32484030
Acute hepatitis C 18.40 14.59 6 18176 181 32495163
Pulmonary tuberculosis 18.36 14.59 18 18164 4971 32490373
Retinitis pigmentosa 18.33 14.59 4 18178 23 32495321
Psychotic disorder 18.24 14.59 40 18142 22980 32472364
Cachexia 17.94 14.59 21 18161 7088 32488256
Atypical mycobacterial infection 17.65 14.59 9 18173 871 32494473
Meningomyelocele 17.58 14.59 6 18176 209 32495135
Nephrocalcinosis 17.55 14.59 8 18174 605 32494739
Cardiomyopathy acute 17.42 14.59 4 18178 30 32495314
Tracheal fistula repair 17.39 14.59 3 18179 3 32495341
Cerebral ventricle dilatation 17.06 14.59 9 18173 934 32494410
Intensive care unit acquired weakness 16.97 14.59 9 18173 944 32494400
Congenital cystic kidney disease 16.90 14.59 7 18175 419 32494925
Hepatic failure 16.84 14.59 51 18131 35629 32459715
Vertigo 16.81 14.59 40 18142 24243 32471101
Myelocytosis 16.67 14.59 4 18178 37 32495307
Retinal toxicity 16.67 14.59 7 18175 434 32494910
Meningitis cryptococcal 16.52 14.59 12 18170 2197 32493147
Congenital hydronephrosis 16.48 14.59 8 18174 697 32494647
Abnormal dreams 16.34 14.59 22 18160 8542 32486802
Lymphocytic infiltration 16.31 14.59 8 18174 713 32494631
CD8 lymphocytes increased 16.30 14.59 4 18178 41 32495303
Glycosuria 16.14 14.59 10 18172 1408 32493936
Infusion related reaction 16.09 14.59 3 18179 45596 32449748
Renal failure 15.90 14.59 129 18053 134349 32360995
Lymphogranuloma venereum 15.86 14.59 3 18179 7 32495337
Seborrhoeic dermatitis 15.84 14.59 10 18172 1455 32493889
Fat tissue decreased 15.80 14.59 4 18178 47 32495297
Immune reconstitution inflammatory syndrome associated tuberculosis 15.76 14.59 7 18175 498 32494846
Pancreatitis acute 15.76 14.59 42 18140 27293 32468051
Birth trauma 15.58 14.59 3 18179 8 32495336
Psychomotor retardation 15.47 14.59 13 18169 2942 32492402
Kidney enlargement 15.44 14.59 8 18174 800 32494544
Blood pressure increased 15.44 14.59 13 18169 79341 32416003
Febrile neutropenia 15.42 14.59 27 18155 119539 32375805
Tracheal deviation 15.32 14.59 3 18179 9 32495335
Oxygen saturation decreased 15.29 14.59 4 18178 48095 32447249
Subacute combined cord degeneration 15.12 14.59 5 18177 158 32495186
Rash maculo-papular 15.10 14.59 42 18140 27980 32467364
Glucose tolerance impaired 14.99 14.59 13 18169 3070 32492274
Drug ineffective 14.90 14.59 140 18042 383337 32112007
Congenital ureteric anomaly 14.84 14.59 4 18178 61 32495283
Hepatitis B 14.79 14.59 18 18164 6323 32489021
Hepatorenal syndrome 14.60 14.59 12 18170 2633 32492711

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 anti-virus drug

Drug Use (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

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 0006-0473 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 0006-3080 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 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