raltegravir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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: OFP
    • 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) 1 Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 9 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 25.72 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 31.80 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility) 71 mg/mL Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma) 0.15 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,MAPK7,PDK1,PDK2,PIK3CB,PRKDC,TEK 15
kinase-selectivity-class EIF2AK3,GRK2 2
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 27.669 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 1
rat-kpuu-brain Rat brain Kpuu 0.030 % High 1

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 1154.42 25.27 565 10472 237845 90379565
Foetal exposure during pregnancy 807.10 25.27 271 10766 42704 90574706
Virologic failure 433.18 25.27 90 10947 2134 90615276
Abortion spontaneous 416.84 25.27 178 10859 53878 90563532
Maternal exposure during pregnancy 402.18 25.27 339 10698 359724 90257686
Premature baby 245.38 25.27 98 10939 24979 90592431
Pathogen resistance 242.29 25.27 73 10964 8042 90609368
Immune reconstitution inflammatory syndrome 235.05 25.27 69 10968 6950 90610460
Viral mutation identified 221.28 25.27 51 10986 1974 90615436
Blood HIV RNA increased 193.71 25.27 39 10998 785 90616625
Caesarean section 186.58 25.27 74 10963 18503 90598907
Lipodystrophy acquired 170.07 25.27 39 10998 1475 90615935
Treatment noncompliance 164.01 25.27 93 10944 51634 90565776
Drug reaction with eosinophilia and systemic symptoms 152.29 25.27 83 10954 42675 90574735
Premature labour 150.98 25.27 58 10979 13318 90604092
Abortion induced 143.00 25.27 54 10983 11834 90605576
Premature delivery 142.93 25.27 77 10960 38685 90578725
Viral load increased 137.52 25.27 33 11004 1523 90615887
Spina bifida 133.56 25.27 29 11008 851 90616559
Congenital genital malformation 130.97 25.27 22 11015 151 90617259
Drug resistance 116.49 25.27 62 10975 30387 90587023
Ectopic kidney 104.62 25.27 16 11021 54 90617356
Renal dysplasia 101.23 25.27 20 11017 364 90617046
Genotype drug resistance test positive 98.11 25.27 20 11017 429 90616981
Drug interaction 98.04 25.27 143 10894 276310 90341100
Cloacal exstrophy 97.52 25.27 17 11020 149 90617261
Foetal growth restriction 92.88 25.27 37 11000 9343 90608067
Bladder agenesis 91.50 25.27 16 11021 143 90617267
Genitalia external ambiguous 90.81 25.27 16 11021 150 90617260
Caudal regression syndrome 87.92 25.27 16 11021 183 90617227
Gastrointestinal disorder congenital 85.69 25.27 15 11022 135 90617275
Sudden infant death syndrome 85.66 25.27 17 11020 317 90617093
Tethered cord syndrome 81.68 25.27 16 11021 278 90617132
Anal atresia 80.60 25.27 17 11020 433 90616977
Gastrointestinal malformation 80.51 25.27 15 11022 197 90617213
Meconium stain 80.37 25.27 15 11022 199 90617211
Meningomyelocele 80.00 25.27 18 11019 624 90616786
Foetal death 78.70 25.27 42 10995 20681 90596729
Premature rupture of membranes 76.94 25.27 28 11009 5530 90611880
Hepatocellular injury 75.75 25.27 46 10991 28912 90588498
Hepatic cytolysis 75.50 25.27 47 10990 30869 90586541
Immune reconstitution inflammatory syndrome associated tuberculosis 73.12 25.27 16 11021 487 90616923
Congenital heart valve disorder 72.97 25.27 12 11025 71 90617339
Exomphalos 71.15 25.27 16 11021 553 90616857
Gastroschisis 70.35 25.27 15 11022 403 90617007
Neonatal respiratory arrest 70.26 25.27 11 11026 45 90617365
Umbilical cord abnormality 68.27 25.27 16 11021 666 90616744
Pre-eclampsia 67.64 25.27 31 11006 11017 90606393
Central obesity 66.18 25.27 18 11019 1372 90616038
Alanine aminotransferase increased 64.95 25.27 76 10961 118262 90499148
Cholestasis of pregnancy 63.93 25.27 18 11019 1559 90615851
Complication of delivery 62.86 25.27 12 11025 181 90617229
Hepatitis C 61.92 25.27 24 11013 5636 90611774
Hemivertebra 61.09 25.27 11 11026 118 90617292
Congenital pulmonary valve disorder 60.55 25.27 10 11027 61 90617349
Pain 60.53 25.27 23 11014 996318 89621092
Maternal drugs affecting foetus 60.47 25.27 23 11014 5132 90612278
Bacterial vulvovaginitis 59.36 25.27 15 11022 858 90616552
Aspartate aminotransferase increased 57.97 25.27 67 10970 102870 90514540
Bacillus infection 57.96 25.27 15 11022 944 90616466
Hydrocephalus 56.74 25.27 23 11014 6071 90611339
Single functional kidney 56.04 25.27 12 11025 329 90617081
Neural tube defect 55.84 25.27 11 11026 197 90617213
Cardiac murmur 55.70 25.27 32 11005 18162 90599248
CD4 lymphocytes decreased 55.27 25.27 16 11021 1531 90615879
Foetal growth abnormality 53.93 25.27 9 11028 59 90617351
Stillbirth 52.30 25.27 23 11014 7420 90609990
Pulmonary valve sclerosis 51.65 25.27 8 11029 30 90617380
Live birth 50.54 25.27 55 10982 79052 90538358
Congenital choroid plexus cyst 50.48 25.27 11 11026 328 90617082
Low birth weight baby 50.04 25.27 24 11013 9443 90607967
Ultrasound antenatal screen 48.99 25.27 10 11027 216 90617194
Hyperbilirubinaemia 46.68 25.27 26 11011 13910 90603500
Mycoplasma genitalium infection 46.39 25.27 7 11030 21 90617389
Generalised anxiety disorder 46.23 25.27 16 11021 2731 90614679
Atrial septal defect 43.90 25.27 21 11016 8213 90609197
Anaemia 43.42 25.27 117 10920 352685 90264725
Congenital ectopic bladder 42.94 25.27 8 11029 105 90617305
Renal aplasia 42.67 25.27 10 11027 416 90616994
Trisomy 21 41.95 25.27 10 11027 448 90616962
Renal tubular dysfunction 40.82 25.27 10 11027 503 90616907
Antiviral drug level below therapeutic 40.40 25.27 7 11030 59 90617351
Ventricular hypertrophy 39.31 25.27 15 11022 3376 90614034
Cushingoid 39.27 25.27 21 11016 10374 90607036
Gestational diabetes 38.92 25.27 21 11016 10561 90606849
Viral load decreased 38.84 25.27 6 11031 22 90617388
Oesophageal candidiasis 38.19 25.27 18 11019 6811 90610599
Anencephaly 38.07 25.27 9 11028 389 90617021
Hepatitis fulminant 37.11 25.27 15 11022 3930 90613480
CSF HIV escape syndrome 36.89 25.27 7 11030 102 90617308
Product size issue 36.68 25.27 9 11028 456 90616954
Congenital anomaly 36.33 25.27 17 11020 6330 90611080
Large for dates baby 35.69 25.27 9 11028 510 90616900
Plagiocephaly 35.61 25.27 7 11030 124 90617286
Hepatitis B DNA increased 35.42 25.27 8 11029 282 90617128
Nephropathy toxic 35.36 25.27 21 11016 12667 90604743
Abdominal discomfort 34.38 25.27 8 11029 477320 90140090
Sepsis neonatal 34.21 25.27 9 11028 604 90616806
Arthralgia 34.11 25.27 27 11010 778495 89838915
Fatigue 33.34 25.27 56 10981 1153967 89463443
Systemic lupus erythematosus 33.09 25.27 3 11034 361893 90255517
Drug hypersensitivity 32.93 25.27 8 11029 463601 90153809
Drug ineffective 32.43 25.27 76 10961 1384222 89233188
Congenital hydrocephalus 32.08 25.27 7 11030 210 90617200
Dyspnoea 31.12 25.27 37 11000 880918 89736492
Mitochondrial cytopathy 31.10 25.27 7 11030 243 90617167
Fall 31.09 25.27 10 11027 481800 90135610
Small for dates baby 30.49 25.27 14 11023 4993 90612417
Thymus hypoplasia 30.49 25.27 5 11032 29 90617381
Eosinophilia 29.82 25.27 26 11011 28507 90588903
Congenital absence of bile ducts 29.80 25.27 5 11032 34 90617376
Hydrops foetalis 29.47 25.27 8 11029 605 90616805
Diastasis recti abdominis 29.43 25.27 5 11032 37 90617373
Congenital aortic stenosis 29.43 25.27 5 11032 37 90617373
Heart disease congenital 29.28 25.27 10 11027 1639 90615771
Dermatitis exfoliative 29.15 25.27 14 11023 5522 90611888
Alopecia 29.03 25.27 12 11025 495059 90122351
Hepatitis cholestatic 28.75 25.27 16 11021 8545 90608865
Cholestasis 28.13 25.27 28 11009 36271 90581139
Furuncle 27.79 25.27 15 11022 7546 90609864
Hepatotoxicity 27.76 25.27 31 11006 45811 90571599
Chronic papillomatous dermatitis 27.57 25.27 5 11032 56 90617354
Nasopharyngitis 27.06 25.27 8 11029 407096 90210314
Mental disability 27.04 25.27 6 11031 195 90617215
Microcephaly 26.97 25.27 9 11028 1375 90616035
Amniotic cavity infection 26.90 25.27 9 11028 1387 90616023
Renal failure 26.65 25.27 53 10984 130954 90486456
Hepatic failure 26.02 25.27 28 11009 39700 90577710
Contraindicated product administered 25.94 25.27 4 11033 320135 90297275
Hand deformity 25.68 25.27 3 11034 296359 90321051
Hepatitis B 25.54 25.27 12 11025 4507 90612903
Congenital intestinal malformation 25.52 25.27 5 11032 87 90617323
Patent ductus arteriosus 25.42 25.27 12 11025 4557 90612853
Rash maculo-papular 25.33 25.27 28 11009 40905 90576505

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 1179.11 15.30 1029 21380 265970 42332956
Depression 1178.08 15.30 729 21680 110634 42488292
Virologic failure 570.90 15.30 168 22241 3826 42595100
Psychiatric decompensation 566.03 15.30 169 22240 4053 42594873
Depression suicidal 448.46 15.30 133 22276 3112 42595814
Lipodystrophy acquired 436.12 15.30 132 22277 3318 42595608
Tearfulness 429.97 15.30 131 22278 3369 42595557
Pathogen resistance 417.98 15.30 174 22235 11276 42587650
Immune reconstitution inflammatory syndrome 414.08 15.30 167 22242 9976 42588950
Depressive symptom 392.66 15.30 125 22284 3728 42595198
Foetal exposure during pregnancy 359.88 15.30 253 22156 47058 42551868
Psychomotor skills impaired 329.20 15.30 118 22291 5086 42593840
Mitochondrial toxicity 308.94 15.30 95 22314 2520 42596406
Paranoia 297.70 15.30 146 22263 13880 42585046
Blood HIV RNA increased 294.97 15.30 82 22327 1509 42597417
Viral mutation identified 282.34 15.30 94 22315 3237 42595689
Progressive external ophthalmoplegia 281.34 15.30 77 22332 1334 42597592
Loss of personal independence in daily activities 277.37 15.30 221 22188 49595 42549331
Eyelid ptosis 232.20 15.30 98 22311 6563 42592363
Suicidal ideation 202.84 15.30 182 22227 47979 42550947
Psychotic disorder 191.80 15.30 143 22266 29065 42569861
Drug resistance 184.26 15.30 149 22260 34099 42564827
Viral load increased 127.96 15.30 51 22358 2946 42595980
Volvulus 124.85 15.30 45 22364 1968 42596958
CD4 lymphocytes decreased 111.89 15.30 41 22368 1880 42597046
Renal tubular disorder 106.80 15.30 52 22357 4857 42594069
Diplopia 106.29 15.30 87 22322 20229 42578697
HIV-associated neurocognitive disorder 103.07 15.30 26 22383 322 42598604
Hepatitis C 90.68 15.30 60 22349 10073 42588853
Psychomotor retardation 87.96 15.30 44 22365 4355 42594571
CSF HIV escape syndrome 84.30 15.30 20 22389 188 42598738
Dyslipidaemia 80.03 15.30 54 22355 9364 42589562
Prescribed overdose 79.72 15.30 61 22348 12866 42586060
Anxiety 77.83 15.30 184 22225 118376 42480550
Genotype drug resistance test positive 74.98 15.30 27 22382 1177 42597749
Brachydactyly 74.33 15.30 18 22391 186 42598740
Drug reaction with eosinophilia and systemic symptoms 73.12 15.30 100 22309 41975 42556951
Brain stem stroke 69.35 15.30 19 22390 330 42598596
Ultrasound antenatal screen 68.77 15.30 21 22388 543 42598383
Trisomy 18 67.71 15.30 23 22386 842 42598084
Gene mutation 64.71 15.30 27 22382 1754 42597172
Ophthalmoplegia 62.40 15.30 28 22381 2172 42596754
Cleft lip and palate 62.20 15.30 22 22387 910 42598016
Osteoporotic fracture 62.03 15.30 25 22384 1486 42597440
Hydrops foetalis 59.02 15.30 21 22388 884 42598042
Osteoporosis 56.19 15.30 53 22356 14853 42584073
Hemivertebra 53.71 15.30 13 22396 134 42598792
Oesophageal atresia 53.20 15.30 17 22392 512 42598414
Dyspnoea 50.37 15.30 98 22311 442523 42156403
Renal impairment 48.89 15.30 148 22261 110080 42488846
Gastrointestinal tube insertion 48.58 15.30 21 22388 1489 42597437
Treatment noncompliance 47.43 15.30 77 22332 37595 42561331
Phalangeal hypoplasia 44.76 15.30 10 22399 70 42598856
Genital herpes 43.40 15.30 16 22393 746 42598180
Hepatitis cholestatic 43.02 15.30 38 22371 9786 42589140
Cytomegalovirus chorioretinitis 42.95 15.30 28 22381 4583 42594343
Drug level decreased 42.52 15.30 38 22371 9939 42588987
Hypotension 42.17 15.30 44 22365 257587 42341339
Pneumonia 41.76 15.30 101 22308 422048 42176878
Genital herpes simplex 39.85 15.30 10 22399 121 42598805
Syphilis 39.84 15.30 14 22395 568 42598358
Treatment failure 39.74 15.30 96 22313 62528 42536398
Anogenital dysplasia 39.05 15.30 10 22399 132 42598794
Laryngomalacia 38.73 15.30 12 22397 326 42598600
Fanconi syndrome acquired 36.43 15.30 19 22390 2051 42596875
Osteonecrosis 35.89 15.30 43 22366 15822 42583104
Premature baby 35.71 15.30 52 22357 23101 42575825
Oesophageal candidiasis 35.64 15.30 27 22382 5608 42593318
Anal cancer 34.97 15.30 12 22397 453 42598473
Atrial fibrillation 34.65 15.30 15 22394 139578 42459348
Hepatic cirrhosis 34.47 15.30 47 22362 19655 42579271
Acquired immunodeficiency syndrome 33.93 15.30 12 22397 496 42598430
Incorrect route of product administration 33.79 15.30 52 22357 24253 42574673
Urinary tract inflammation 33.53 15.30 10 22399 238 42598688
Blood creatine phosphokinase increased 32.72 15.30 76 22333 48262 42550664
Abortion spontaneous 32.63 15.30 11 22398 393 42598533
Superior mesenteric artery syndrome 31.79 15.30 8 22401 98 42598828
Drug abuse 31.70 15.30 8 22401 104763 42494163
Multiple-drug resistance 31.42 15.30 28 22381 7294 42591632
Drug ineffective 31.28 15.30 199 22210 629998 41968928
COVID-19 31.18 15.30 11 22398 115937 42482989
HIV lipodystrophy 30.76 15.30 6 22403 19 42598907
Polydactyly 29.66 15.30 14 22395 1220 42597706
Back pain 29.64 15.30 19 22390 141757 42457169
Malignant neoplasm progression 29.64 15.30 10 22399 108390 42490536
Chronic hepatitis C 29.53 15.30 11 22398 528 42598398
Congenital mitral valve incompetence 29.42 15.30 8 22401 135 42598791
Intestinal malrotation 29.28 15.30 6 22403 26 42598900
Progressive multifocal leukoencephalopathy 28.98 15.30 33 22376 11503 42587423
Glucose tolerance impaired 28.86 15.30 21 22388 4103 42594823
Dysphagia 27.97 15.30 93 22316 72626 42526300
Congenital foot malformation 27.92 15.30 10 22399 429 42598497
Disease progression 27.72 15.30 21 22388 143635 42455291
Nephropathy toxic 27.70 15.30 39 22370 16799 42582127
Lipohypertrophy 27.47 15.30 9 22400 294 42598632
Constipation 27.34 15.30 27 22382 162264 42436662
Confusional state 26.97 15.30 29 22380 167568 42431358
Adrenal suppression 26.47 15.30 12 22397 953 42597973
Completed suicide 26.20 15.30 9 22400 96456 42502470
HIV associated nephropathy 26.10 15.30 9 22400 345 42598581
Blood bilirubin increased 25.97 15.30 64 22345 42188 42556738
Exposure during pregnancy 25.92 15.30 27 22382 8521 42590405
Congenital skin dimples 25.90 15.30 8 22401 215 42598711
Low birth weight baby 25.90 15.30 29 22380 9926 42589000
Pain 25.41 15.30 57 22352 244791 42354135
Adverse event 25.35 15.30 45 22364 23595 42575331
Haemophilic arthropathy 24.75 15.30 8 22401 250 42598676
HIV infection 24.35 15.30 13 22396 1472 42597454
Laryngectomy 23.97 15.30 4 22405 3 42598923
Febrile neutropenia 23.86 15.30 38 22371 185665 42413261
Acquired gene mutation 23.59 15.30 13 22396 1567 42597359
Respiratory failure 23.13 15.30 20 22389 128112 42470814
Off label use 23.00 15.30 220 22189 638115 41960811
Strongyloidiasis 22.94 15.30 17 22392 3414 42595512
Conductive deafness 22.77 15.30 9 22400 508 42598418
Mycobacterium avium complex infection 22.52 15.30 16 22393 3011 42595915
Hypersplenism 22.41 15.30 9 22400 530 42598396
Blood pressure increased 22.21 15.30 13 22396 101915 42497011
Cystitis noninfective 22.17 15.30 9 22400 545 42598381
Erosive duodenitis 22.08 15.30 13 22396 1776 42597150
Infusion related reaction 21.89 15.30 3 22406 60803 42538123
Condition aggravated 21.52 15.30 68 22341 260686 42338240
Congenital vesicoureteric reflux 21.47 15.30 5 22404 43 42598883
Oxygen saturation decreased 21.47 15.30 4 22405 64683 42534243
Heart transplant rejection 21.21 15.30 12 22397 1522 42597404
Drug hypersensitivity 21.21 15.30 13 22396 99376 42499550
Enanthema 20.98 15.30 9 22400 626 42598300
Drug level increased 20.89 15.30 44 22365 26156 42572770
Acute hepatitis C 20.61 15.30 6 22403 131 42598795
Lipoatrophy 20.49 15.30 8 22401 437 42598489
Injection site pain 20.46 15.30 3 22406 57795 42541131
Therapeutic product effect incomplete 20.36 15.30 6 22403 70933 42527993
Sepsis 20.19 15.30 47 22362 199287 42399639
Hepatic cytolysis 20.16 15.30 44 22365 26800 42572126
Lipids abnormal 20.10 15.30 8 22401 460 42598466
White matter lesion 20.00 15.30 10 22399 988 42597938
Pulmonary tuberculosis 19.66 15.30 19 22390 5482 42593444
Antiviral drug level above therapeutic 19.53 15.30 5 22404 66 42598860
Liver disorder 19.24 15.30 55 22354 39589 42559337
Maternal drugs affecting foetus 19.15 15.30 16 22393 3823 42595103
Retinitis pigmentosa 19.05 15.30 4 22405 20 42598906
Wheezing 19.03 15.30 3 22406 54778 42544148
Peripheral swelling 18.99 15.30 12 22397 90258 42508668
Chest discomfort 18.96 15.30 5 22404 63611 42535315
Myalgia 18.86 15.30 100 22309 95980 42502946
Jaundice 18.78 15.30 50 22359 34539 42564387
Hepatitis 18.55 15.30 43 22366 27257 42571669
Aspartate aminotransferase increased 18.48 15.30 85 22324 77078 42521848
Immune reconstitution inflammatory syndrome associated tuberculosis 18.43 15.30 8 22401 573 42598353
Hyperbilirubinaemia 18.04 15.30 36 22373 20599 42578327
Portal hypertension 18.00 15.30 17 22392 4770 42594156
Diet noncompliance 17.89 15.30 6 22403 211 42598715
Intentional product use issue 17.85 15.30 80 22329 71753 42527173
Hyperphagia 17.69 15.30 11 22398 1659 42597267
Intensive care unit acquired weakness 17.68 15.30 10 22399 1268 42597658
Congenital syphilis 17.58 15.30 3 22406 3 42598923
Tracheal fistula repair 17.58 15.30 3 22406 3 42598923
Meningomyelocele 17.55 15.30 6 22403 224 42598702
Hepatic enzyme decreased 17.49 15.30 5 22404 102 42598824
Hypertriglyceridaemia 17.47 15.30 24 22385 10102 42588824
Varices oesophageal 17.37 15.30 16 22393 4349 42594577
Cholestasis 17.32 15.30 47 22362 32832 42566094
Erythema 17.29 15.30 19 22390 108774 42490152
Liver transplant 17.25 15.30 13 22396 2678 42596248
Dizziness 17.24 15.30 70 22339 249184 42349742
Pancreatitis 17.22 15.30 56 22353 43212 42555714
Myelocytosis 17.11 15.30 4 22405 35 42598891
Congenital renal disorder 17.09 15.30 5 22404 111 42598815
Glycosuria 17.03 15.30 10 22399 1360 42597566
Choroiditis 17.00 15.30 10 22399 1365 42597561
Hyperlactacidaemia 16.90 15.30 16 22393 4500 42594426
Congenital cystic kidney disease 16.83 15.30 7 22402 451 42598475
Cerebral ventricle dilatation 16.77 15.30 9 22400 1030 42597896
Pancreatitis acute 16.71 15.30 47 22362 33517 42565409
Haematochezia 16.66 15.30 5 22404 58431 42540495
Abnormal dreams 16.42 15.30 21 22388 8250 42590676
Intentional product misuse 16.42 15.30 6 22403 61894 42537032
Heart rate increased 16.23 15.30 4 22405 53251 42545675
Renal failure 16.16 15.30 130 22279 143596 42455330
Birth trauma 16.05 15.30 3 22406 7 42598919
Congenital hydronephrosis 16.01 15.30 8 22401 789 42598137
Dermatitis exfoliative 15.99 15.30 19 22390 6928 42591998
Nephrocalcinosis 15.96 15.30 8 22401 795 42598131
Adrenogenital syndrome 15.90 15.30 4 22405 49 42598877
Retinal toxicity 15.88 15.30 7 22402 520 42598406
Nephrolithiasis 15.88 15.30 49 22360 36781 42562145
Hyperlipidaemia 15.86 15.30 35 22374 21481 42577445
Myopathy 15.80 15.30 27 22382 13734 42585192
Hepatic failure 15.79 15.30 50 22359 38050 42560876
Subacute combined cord degeneration 15.67 15.30 5 22404 150 42598776
Dehydration 15.52 15.30 32 22377 141735 42457191
Productive cough 15.47 15.30 4 22405 51563 42547363
VACTERL syndrome 15.47 15.30 4 22405 55 42598871
Alanine aminotransferase increased 15.34 15.30 89 22320 88317 42510609

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 1263.93 16.56 282 26172 4670 110558175
Drug interaction 1202.00 16.56 974 25480 499209 110063636
Pathogen resistance 845.43 16.56 267 26187 17405 110545440
Depression 734.14 16.56 606 25848 316729 110246116
Psychiatric decompensation 674.55 16.56 175 26279 5590 110557255
Viral mutation identified 669.89 16.56 165 26289 4254 110558591
Blood HIV RNA increased 621.04 16.56 136 26318 2052 110560793
Immune reconstitution inflammatory syndrome 596.99 16.56 201 26253 16025 110546820
Lipodystrophy acquired 561.75 16.56 144 26310 4380 110558465
Depression suicidal 495.11 16.56 132 26322 4692 110558153
Tearfulness 439.33 16.56 132 26322 7263 110555582
Depressive symptom 401.69 16.56 127 26327 8287 110554558
Psychomotor skills impaired 389.34 16.56 119 26335 6939 110555906
Mitochondrial toxicity 362.63 16.56 95 26359 3150 110559695
Progressive external ophthalmoplegia 346.50 16.56 78 26376 1342 110561503
Paranoia 339.11 16.56 145 26309 22229 110540616
Drug resistance 329.36 16.56 191 26263 56183 110506662
Abortion spontaneous 323.99 16.56 160 26294 34122 110528723
Viral load increased 238.51 16.56 69 26385 3321 110559524
Foetal exposure during pregnancy 233.29 16.56 82 26372 7423 110555422
Eyelid ptosis 230.83 16.56 95 26359 13232 110549613
Psychotic disorder 226.62 16.56 145 26309 50792 110512053
Exposure during pregnancy 223.38 16.56 236 26218 167188 110395657
Loss of personal independence in daily activities 211.82 16.56 218 26236 149802 110413043
Maternal exposure during pregnancy 207.18 16.56 279 26175 254604 110308241
Drug reaction with eosinophilia and systemic symptoms 206.24 16.56 165 26289 81930 110480915
Suicidal ideation 200.96 16.56 172 26282 93765 110469080
Treatment noncompliance 150.71 16.56 131 26323 72859 110489986
Genotype drug resistance test positive 146.74 16.56 39 26415 1367 110561478
Hepatitis C 144.02 16.56 67 26387 12506 110550339
HIV-associated neurocognitive disorder 141.96 16.56 30 26424 378 110562467
Caesarean section 135.00 16.56 66 26388 13751 110549094
CD4 lymphocytes decreased 130.03 16.56 42 26412 2932 110559913
CSF HIV escape syndrome 128.52 16.56 27 26427 330 110562515
Diplopia 117.70 16.56 90 26364 41804 110521041
Ultrasound antenatal screen 115.29 16.56 28 26426 678 110562167
Renal tubular disorder 112.04 16.56 48 26406 7381 110555464
Abortion induced 108.51 16.56 48 26406 7971 110554874
Hydrops foetalis 107.48 16.56 27 26427 754 110562091
Cleft lip and palate 99.22 16.56 25 26429 707 110562138
Trisomy 18 98.20 16.56 24 26430 597 110562248
Renal impairment 97.06 16.56 167 26287 188278 110374567
Psychomotor retardation 97.00 16.56 44 26410 7748 110555097
Gene mutation 93.47 16.56 34 26420 3395 110559450
Premature labour 90.16 16.56 44 26410 9128 110553717
Dyslipidaemia 87.65 16.56 52 26402 15913 110546932
Immune reconstitution inflammatory syndrome associated tuberculosis 81.07 16.56 23 26431 1031 110561814
Pain 80.99 16.56 66 26388 954889 109607956
Hepatitis cholestatic 78.07 16.56 50 26404 17516 110545329
Premature delivery 77.79 16.56 62 26392 30570 110532275
Hepatic cytolysis 77.59 16.56 80 26374 54973 110507872
Nephropathy toxic 77.10 16.56 59 26395 27419 110535426
Joint swelling 70.19 16.56 11 26443 442834 110120011
Aspartate aminotransferase increased 69.90 16.56 132 26322 159804 110403041
Brain stem stroke 69.01 16.56 19 26435 762 110562083
Ophthalmoplegia 67.26 16.56 27 26427 3523 110559322
Hyperbilirubinaemia 67.24 16.56 57 26397 30614 110532231
Alanine aminotransferase increased 65.15 16.56 139 26315 183634 110379211
Peripheral swelling 64.11 16.56 10 26444 404024 110158821
Spina bifida 61.21 16.56 13 26441 168 110562677
Drug hypersensitivity 60.25 16.56 17 26437 454073 110108772
Renal failure 60.16 16.56 153 26301 226421 110336424
Syphilis 60.03 16.56 17 26437 757 110562088
Oesophageal candidiasis 59.25 16.56 36 26418 11498 110551347
Anxiety 58.91 16.56 199 26255 344879 110217966
Genital herpes 57.52 16.56 22 26432 2525 110560320
Premature rupture of membranes 57.14 16.56 26 26428 4611 110558234
Osteoporotic fracture 56.68 16.56 27 26427 5310 110557535
Cytomegalovirus chorioretinitis 54.90 16.56 29 26425 7099 110555746
Central obesity 54.80 16.56 20 26434 2016 110560829
Hepatocellular injury 54.69 16.56 64 26390 50578 110512267
Pulmonary tuberculosis 53.41 16.56 31 26423 9108 110553737
Premature baby 52.90 16.56 25 26429 4830 110558015
Dyspnoea 52.64 16.56 117 26337 1106755 109456090
Fanconi syndrome acquired 50.40 16.56 21 26433 3013 110559832
Abdominal discomfort 49.96 16.56 16 26438 393842 110169003
Multiple-drug resistance 49.90 16.56 34 26420 13201 110549644
Bacterial vulvovaginitis 48.79 16.56 14 26440 654 110562191
Cushingoid 48.76 16.56 32 26422 11680 110551165
Foetal death 48.45 16.56 36 26418 16009 110546836
Renal dysplasia 47.73 16.56 9 26445 60 110562785
Infection 47.22 16.56 14 26440 362186 110200659
Adrenal suppression 46.91 16.56 17 26437 1679 110561166
Gastroschisis 46.46 16.56 8 26446 29 110562816
Stillbirth 43.55 16.56 21 26433 4243 110558602
Lower respiratory tract infection 43.50 16.56 4 26450 243102 110319743
Systemic lupus erythematosus 43.41 16.56 5 26449 254333 110308512
Confusional state 42.69 16.56 30 26424 468650 110094195
Dermatitis exfoliative 42.42 16.56 29 26425 11318 110551527
Liver transplant 42.08 16.56 21 26433 4568 110558277
Nasopharyngitis 41.89 16.56 21 26433 394340 110168505
Mycoplasma genitalium infection 41.67 16.56 7 26447 21 110562824
Mitochondrial cytopathy 41.43 16.56 11 26443 384 110562461
Foetal growth abnormality 40.96 16.56 7 26447 24 110562821
Progressive multifocal leukoencephalopathy 40.19 16.56 39 26415 24917 110537928
Contraindicated product administered 39.69 16.56 6 26448 248261 110314584
Sinusitis 39.53 16.56 11 26443 296677 110266168
Alopecia 39.38 16.56 19 26435 364734 110198111
Blood creatine phosphokinase increased 39.21 16.56 66 26388 73011 110489834
Cachexia 38.86 16.56 29 26425 12976 110549869
Generalised anxiety disorder 38.78 16.56 17 26437 2762 110560083
Asthma 37.90 16.56 7 26447 250284 110312561
Hepatitis B DNA increased 37.07 16.56 12 26442 843 110562002
Urticaria 36.95 16.56 15 26439 318842 110244003
Cholestasis 36.94 16.56 60 26394 64458 110498387
Wound 36.72 16.56 6 26448 234431 110328414
Bacillus infection 36.66 16.56 14 26440 1600 110561245
Urinary tract inflammation 36.64 16.56 10 26444 388 110562457
Therapeutic product effect decreased 36.64 16.56 7 26447 244309 110318536
HIV lipodystrophy 36.52 16.56 6 26448 15 110562830
Contusion 36.49 16.56 6 26448 233355 110329490
Antiviral drug level below therapeutic 36.23 16.56 7 26447 54 110562791
Impaired healing 35.84 16.56 3 26451 196714 110366131
Arthralgia 34.90 16.56 85 26369 779547 109783298
Mycobacterium avium complex infection 34.51 16.56 20 26434 5857 110556988
Pancreatitis acute 34.44 16.56 56 26398 60218 110502627
Conductive deafness 34.32 16.56 9 26445 299 110562546
Genital herpes simplex 33.77 16.56 10 26444 522 110562323
Osteonecrosis 33.73 16.56 41 26413 33700 110529145
Pericarditis 33.45 16.56 6 26448 219108 110343737
Drug intolerance 33.24 16.56 29 26425 406483 110156362
Pancytopenia 33.22 16.56 118 26336 209495 110353350
Mobility decreased 33.16 16.56 8 26446 237414 110325431
Acquired immunodeficiency syndrome 32.98 16.56 9 26445 349 110562496
HIV associated nephropathy 32.88 16.56 9 26445 353 110562492
Hepatic failure 32.86 16.56 59 26395 68680 110494165
General physical health deterioration 32.82 16.56 32 26422 425263 110137582
Musculoskeletal stiffness 32.69 16.56 13 26441 279809 110283036
Renal tubular dysfunction 32.61 16.56 11 26443 879 110561966
White matter lesion 32.54 16.56 15 26439 2739 110560106
Helicobacter infection 32.52 16.56 3 26451 181874 110380971
Jaundice 32.45 16.56 54 26400 59182 110503663
Completed suicide 32.26 16.56 9 26445 242372 110320473
Superior mesenteric artery syndrome 32.14 16.56 8 26446 215 110562630
Strongyloidiasis 32.05 16.56 18 26436 4968 110557877
HIV viraemia 31.28 16.56 7 26447 117 110562728
Swelling 31.26 16.56 23 26431 351018 110211827
Pancreatitis 31.12 16.56 69 26385 93464 110469381
Chronic hepatitis C 31.05 16.56 10 26444 691 110562154
Back pain 30.90 16.56 26 26428 370970 110191875
Face oedema 30.78 16.56 39 26415 33430 110529415
Therapeutic product effect incomplete 30.37 16.56 8 26446 223797 110339048
Enanthema 30.00 16.56 11 26443 1123 110561722
Pain in extremity 29.77 16.56 44 26410 487074 110075771
Pre-eclampsia 29.74 16.56 21 26433 8629 110554216
Single functional kidney 29.52 16.56 8 26446 302 110562543
Acquired gene mutation 29.45 16.56 14 26440 2740 110560105
Nephrolithiasis 29.34 16.56 55 26399 66157 110496688
Injection site pain 29.13 16.56 4 26450 177918 110384927
Injury 28.99 16.56 4 26450 177261 110385584
Anogenital dysplasia 28.84 16.56 7 26447 169 110562676
Erosive duodenitis 28.71 16.56 13 26441 2278 110560567
HIV infection 28.51 16.56 11 26443 1292 110561553
Prescribed overdose 28.46 16.56 64 26390 87517 110475328
Congenital intestinal malformation 28.45 16.56 5 26449 21 110562824
Foetal growth restriction 28.09 16.56 14 26440 3036 110559809
Drug level decreased 28.03 16.56 28 26426 18520 110544325
Foetal exposure during delivery 27.91 16.56 5 26449 24 110562821
Hepatitis B 27.76 16.56 21 26433 9591 110553254
COVID-19 27.63 16.56 12 26442 245048 110317797
Lipohypertrophy 27.51 16.56 10 26444 996 110561849
Dysphagia 27.43 16.56 90 26364 153510 110409335
Hepatic cirrhosis 27.30 16.56 54 26400 67572 110495273
Lipids abnormal 27.22 16.56 9 26445 676 110562169
Drug ineffective 26.84 16.56 234 26220 1520306 109042539
Toxic skin eruption 26.80 16.56 33 26421 27482 110535363
Proteinuria 26.79 16.56 40 26414 39978 110522867
Viral load abnormal 26.71 16.56 6 26448 102 110562743
HIV infection CDC category C 26.56 16.56 5 26449 33 110562812
Myocardial infarction 26.15 16.56 103 26351 191980 110370865
Hepatic encephalopathy 26.10 16.56 33 26421 28223 110534622
Chest discomfort 26.02 16.56 5 26449 173843 110389002
Retinal toxicity 25.94 16.56 11 26443 1648 110561197
Anaemia 25.82 16.56 221 26233 546865 110015980
Anal cancer 25.64 16.56 9 26445 810 110562035
Eosinophilia 25.51 16.56 48 26406 57888 110504957
Hepatitis fulminant 25.38 16.56 19 26435 8541 110554304
Tuberculosis 25.34 16.56 26 26428 17748 110545097
Cholestasis of pregnancy 25.28 16.56 10 26444 1255 110561590
Haemolytic anaemia 25.23 16.56 28 26426 20892 110541953
Acute hepatitis C 25.18 16.56 7 26447 291 110562554
Nephrocalcinosis 25.00 16.56 11 26443 1803 110561042
Stomatitis 24.98 16.56 17 26437 270225 110292620
Acute stress disorder 24.76 16.56 8 26446 559 110562286
Atrial fibrillation 24.71 16.56 12 26442 229630 110333215
Oxygen saturation decreased 24.62 16.56 4 26450 156978 110405867
Product use issue 24.56 16.56 23 26431 311672 110251173
Fall 24.53 16.56 69 26385 603413 109959432
Oesophageal carcinoma 24.40 16.56 21 26433 11503 110551342
Blood pressure increased 24.22 16.56 16 26438 258357 110304488
Blood bilirubin increased 24.11 16.56 55 26399 75917 110486928
Renal aplasia 24.01 16.56 6 26448 164 110562681
Chronic kidney disease 23.95 16.56 55 26399 76236 110486609
Dry mouth 23.82 16.56 9 26445 199939 110362906
Condition aggravated 23.70 16.56 93 26361 734743 109828102
Hypertriglyceridaemia 23.70 16.56 24 26430 16130 110546715
Hepatotoxicity 23.65 16.56 49 26405 63351 110499494
Choroiditis 22.93 16.56 10 26444 1605 110561240
Pneumonia 22.88 16.56 120 26334 876594 109686251
Rash maculo-papular 22.74 16.56 53 26401 74169 110488676
Viral load decreased 22.54 16.56 4 26450 18 110562827
Blood creatinine increased 22.46 16.56 95 26359 182794 110380051
Lymphadenopathy 22.27 16.56 48 26406 63787 110499058
Hypotension 21.95 16.56 59 26395 523790 110039055
Discomfort 21.94 16.56 12 26442 214695 110348150
Acute kidney injury 21.77 16.56 240 26214 635190 109927655
Malaise 21.68 16.56 85 26369 671734 109891111
Phalangeal hypoplasia 21.58 16.56 4 26450 24 110562821
Abortion spontaneous incomplete 21.58 16.56 4 26450 24 110562821
Mycobacterium avium complex immune restoration disease 21.58 16.56 4 26450 24 110562821
Constipation 21.19 16.56 33 26421 357753 110205092
Product size issue 20.88 16.56 8 26446 923 110561922
Pneumocystis jirovecii pneumonia 20.83 16.56 37 26417 42698 110520147
Hepatitis acute 20.73 16.56 24 26430 18742 110544103
Blood triglycerides increased 20.62 16.56 27 26427 23899 110538946
Fatigue 20.58 16.56 189 26265 1215769 109347076
Congenital foot malformation 20.36 16.56 4 26450 34 110562811
Drug-induced liver injury 20.23 16.56 69 26385 119998 110442847
Muscle spasms 20.23 16.56 22 26432 278135 110284710
Autoimmune hepatitis 19.93 16.56 21 26433 14783 110548062
Glomerulonephritis 19.87 16.56 13 26441 4717 110558128
Brachydactyly 19.68 16.56 4 26450 41 110562804
Hypoaesthesia 19.56 16.56 28 26426 314195 110248650
Inflammation 19.46 16.56 11 26443 193227 110369618
Hyperlactacidaemia 19.40 16.56 16 26438 8270 110554575
Diabetes mellitus 19.35 16.56 60 26394 99321 110463524
Joint range of motion decreased 19.34 16.56 3 26451 121829 110441016
Intensive care unit acquired weakness 19.31 16.56 10 26444 2349 110560496
Osteoporosis 19.23 16.56 55 26399 87097 110475748
Metabolic syndrome 18.94 16.56 11 26443 3236 110559609
Renal colic 18.90 16.56 11 26443 3247 110559598
Blister 18.84 16.56 16 26438 227360 110335485
Nervous system disorder 18.84 16.56 30 26424 31691 110531154
Stevens-Johnson syndrome 18.38 16.56 37 26417 46864 110515981
Glycosuria 18.29 16.56 10 26444 2620 110560225
Gait inability 18.26 16.56 5 26449 136371 110426474
Polyhydramnios 18.18 16.56 9 26445 1924 110560921
Abdominal pain upper 18.12 16.56 35 26419 349076 110213769
Heart rate increased 17.94 16.56 6 26448 143828 110419017
Glomerulonephritis membranous 17.88 16.56 9 26445 1994 110560851
Incorrect route of product administration 17.75 16.56 44 26410 64017 110498828
Folliculitis 17.67 16.56 9 26445 167644 110395201
Arthritis 17.66 16.56 9 26445 167577 110395268
Lymphopenia 17.34 16.56 33 26421 40137 110522708
C-reactive protein increased 17.26 16.56 16 26438 217903 110344942
Congestive cardiomyopathy 17.09 16.56 19 26435 14200 110548645
Skin striae 17.08 16.56 9 26445 2192 110560653
Glucose tolerance impaired 17.03 16.56 16 26438 9821 110553024
Hepatocellular carcinoma 16.97 16.56 16 26438 9864 110552981
Portal hypertension 16.81 16.56 15 26439 8622 110554223
Drug level increased 16.78 16.56 36 26418 47683 110515162
Rhabdomyolysis 16.73 16.56 65 26389 120336 110442509
CD4 lymphocytes abnormal 16.71 16.56 4 26450 91 110562754
Blood triglycerides abnormal 16.65 16.56 6 26448 583 110562262
Blood cholesterol increased 16.58 16.56 12 26442 184773 110378072

FDA Adverse Event Reporting System (Pediatric)

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
Volvulus 53.22 38.14 18 348 94 113493

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 D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D019380 Anti-HIV Agents
MeSH PA D019428 HIV Integrase Inhibitors
FDA EPC N0000175887 Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:36044 antiviral drug
CHEBI has role CHEBI:64946 anti-HIV agent
CHEBI has role CHEBI:67268 HIV-1 integrase inhibitor

Related Drugs by ATC class:

J05AJ Integrase inhibitors 3 drugs
cabotegravirdolutegravirelvitegravir
J05AR Antivirals for treatment of HIV infections, combinations 19 drugs
abacaviratazanavirbictegravircobicistatdarunavirdolutegravirdoravirineefavirenzelvitegraviremtricitabinelamivudinelopinavir show all 19 →

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

DiseaseRelationSNOMED_IDDOID
Human immunodeficiency virus infection indication 86406008 DOID:526
Disorder of muscle contraindication 129565002 DOID:423
Rhabdomyolysis contraindication 240131006
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 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 MSD SUB MERCK N022145 Oct. 12, 2007 RX TABLET ORAL 8852632 Jan. 28, 2028 TREATMENT OF HIV INFECTION
EQ 400MG BASE ISENTRESS MSD SUB MERCK N022145 Oct. 12, 2007 RX TABLET ORAL 7754731 March 11, 2029 TREATMENT OF HIV INFECTION
EQ 600MG BASE ISENTRESS HD MSD SUB MERCK N022145 May 26, 2017 RX TABLET ORAL 7754731 March 11, 2029 TREATMENT OF HIV INFECTION
EQ 100MG BASE ISENTRESS MSD SUB MERCK N203045 Dec. 21, 2011 RX TABLET, CHEWABLE ORAL 7754731 March 11, 2029 TREATMENT OF HIV INFECTION
EQ 25MG BASE ISENTRESS MSD SUB MERCK N203045 Dec. 21, 2011 RX TABLET, CHEWABLE ORAL 7754731 March 11, 2029 TREATMENT OF HIV INFECTION
EQ 100MG BASE/PACKET ISENTRESS MSD SUB MERCK 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 400MG BASE ISENTRESS MSD SUB MERCK N022145 Oct. 12, 2007 RX TABLET ORAL 8771733 June 2, 2030 TREATMENT OF HIV INFECTION
EQ 600MG BASE ISENTRESS HD MSD SUB MERCK N022145 May 26, 2017 RX TABLET ORAL 8771733 June 2, 2030 TREATMENT OF HIV INFECTION
EQ 100MG BASE ISENTRESS MSD SUB MERCK N203045 Dec. 21, 2011 RX TABLET, CHEWABLE ORAL 8771733 June 2, 2030 TREATMENT OF HIV INFECTION
EQ 600MG BASE ISENTRESS HD MSD SUB MERCK 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
Raltegravir HUMAN PRESCRIPTION DRUG LABEL 1 31722-584 TABLET, FILM COATED 400 mg ORAL ANDA 26 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 50090-1085 TABLET, FILM COATED 400 mg ORAL NDA 29 sections
ISENTRESS HUMAN PRESCRIPTION DRUG LABEL 1 53002-1686 TABLET, FILM COATED 400 mg ORAL NDA 29 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 71205-777 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