raltegravir Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antivirals	2352	518048-05-0

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.80	g	O

ADMET properties:

Property	Value	Reference
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 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

Approvals:

Date	Agency	Company
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
C-C chemokine receptor type 1	GPCR	P32246	CCR1_HUMAN		Ki	8.30	CHEMBL
Integrase	Enzyme		Q7ZJM1_9HIV1	INHIBITOR	IC50	8	CHEMBL	CHEMBL
Gag-Pol polyprotein	Polyprotein		POL_HV1BR	INHIBITOR	IC50	7.52	WOMBAT-PK
Integrase	Enzyme		Q76353_9HIV1		IC50	5.74	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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