OMAPATRILAT

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C19H24N2O4S2
Molecular Weight	408.535
Optical Activity	UNSPECIFIED
Defined Stereocenters	4 / 4
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)[C@@H]1CCC[C@@H]2SCC[C@H](NC(=O)[C@@H](S)CC3=CC=CC=C3)C(=O)N12

InChI

InChIKey=LVRLSYPNFFBYCZ-VGWMRTNUSA-N

InChI=1S/C19H24N2O4S2/c22-17(15(26)11-12-5-2-1-3-6-12)20-13-9-10-27-16-8-4-7-14(19(24)25)21(16)18(13)23/h1-3,5-6,13-16,26H,4,7-11H2,(H,20,22)(H,24,25)/t13-,14-,15-,16-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C19H24N2O4S2
Molecular Weight	408.535
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	4 / 4
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.medscape.com/viewarticle/443224
Curator's Comment: description was created based on several sources, including https://www.drugbank.ca/drugs/DB00886

Omapatrilat is an antihypertensive agent that inhibits both neprilysin (neutral endopeptidase, NEP) and angiotensin-converting enzyme (ACE). The drug was developed for possible use in heart failure and hypertension, but was not approved by the FDA due to angioedema safety concerns.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Angiotensin-converting enzyme 94 Target ID: P12821 Gene ID: 1636.0 Gene Symbol: ACE Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/10856268	Inhibitor 8504		0.06 nM [Ki]
Neprilysin 29 Target ID: CHEMBL1944 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19899765	Inhibitor 8504		9.0 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Heart failure 106 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16086927	Primary	Phase III 665	Unknown Approved Use Unknown
Hypertension 575 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14751650	Primary	Phase III 665	Unknown Approved Use Unknown
Chronic angina pectoris 1 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15904630	Primary	Not Provided 511	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
1.28 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	7.5 mg single, oral dose: 7.5 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
51.09 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
89.29 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
286.35 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
491.61 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1008.92 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
26.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
93.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
181.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
203.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	125 mg 1 times / day multiple, oral dose: 125 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
14.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
80.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
175.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
297.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
895.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	125 mg 1 times / day steady-state, oral dose: 125 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
11.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
16.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
13.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
14.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
11.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
0.43 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.52 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	7.5 mg single, oral dose: 7.5 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
69.19 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
149.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
406.52 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
741.39 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1890.76 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
19.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
63.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
147.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
341.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
369.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	125 mg 1 times / day multiple, oral dose: 125 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
30.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
92.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
226.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
420.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
745.2 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	125 mg 1 times / day steady-state, oral dose: 125 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
11.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
16.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
29.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
19.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
25.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
25.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
17.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11014407/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
19.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
17.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
17.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
14.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12968984/	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	OMAPATRILAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
20% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10968433/			OMAPATRILAT plasma	Homo sapiens

Doses

Dose	Population	Adverse events
500 mg single, oral Highest studied dose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/	Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/
125 mg 1 times / day multiple, oral Dose: 125 mg, 1 times / day Route: oral Route: multiple Dose: 125 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/	DLT: Lethargy, Headache... Dose limiting toxicities: Lethargy (16.7%) Headache Dizziness Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/

AEs

AE	Significance	Dose	Population
Lethargy	16.7% DLT, Disc. AE	125 mg 1 times / day multiple, oral Dose: 125 mg, 1 times / day Route: oral Route: multiple Dose: 125 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/
Dizziness	DLT, Disc. AE	125 mg 1 times / day multiple, oral Dose: 125 mg, 1 times / day Route: oral Route: multiple Dose: 125 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/
Headache	DLT, Disc. AE	125 mg 1 times / day multiple, oral Dose: 125 mg, 1 times / day Route: oral Route: multiple Dose: 125 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12968984/

PubMed

Title	Date	PubMed
Omapatrilat and enalapril in patients with hypertension: the Omapatrilat Cardiovascular Treatment vs. Enalapril (OCTAVE) trial.	2004 Feb	14751650
Effect of bradykinin metabolism inhibitors on evoked hypotension in rats: rank efficacy of enzymes associated with bradykinin-mediated angioedema.	2008 Mar	18084312

Patents

Sample Use Guides

In Vivo Use Guide

In phase III trial, omapatrilat was administered at dose 40 mg every day.

Route of Administration: Oral

In Vitro Use Guide

Inhibition studies of recombinant angiotensin-converting enzyme (ACE) and were performed with the use of Ang I, HHL, and the new synthetic peptide AcSDAcKP as substrates. The inhibitory potency of omapatrilat and toward recombinant wild-type ACE was determined by establishing dose dependent inhibition curves at equilibrium. Inhibition of Ang I, HHL, and AcSDAcKP hydrolysis was determined with the use of 0.1 nmol/L, 0.1 nmol/L, and 0.4 nmol/L of wild-type ACE respectively. After preincubation with 0.05 to 2.5 nmol/L of inhibitor at 37°C for 1 hour, reactions were initiated by substrate addition at 2 different concentrations (0.53Km and 33Km) and performed for 5, 10, 30, and 60 minutes. The rate of hydrolysis of all the substrates used was quantified by high-performance liquid chromatography.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:12:39 GMT 2025` Edited by `admin` on `Mon Mar 31 18:12:39 GMT 2025`
Record UNII	36NLI90E7T
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

OMAPATRILAT

Official Name

English

BMS-186716

Preferred Name

English

omapatrilat [INN]

Common Name

English

OMAPATRILATE

Common Name

English

OMAPATRILAT [USAN]

Common Name

English

OMAPATRILAT [MART.]

Common Name

English

BMS-186716-01

Code

English

(4S-(4.ALPHA.(R*),7.ALPHA.,10A.BETA.))-OCTAHYDRO-4-((2-MERCAPTO-1-OXO-3-PHENYLPROPYL)AMINO)-5-OXO-7H-PYRIDO(2,1-B)(1,3)THIAZEPINE-7-CARBOXYLIC ACID

Common Name

English

OMAPATRILAT [VANDF]

Common Name

English

Omapatrilat [WHO-DD]

Common Name

English

OMAPATRILAT [MI]

Common Name

English

(4S,7S,10aS)-Octahydro-4-[(S)-?-mercaptohydrocinnamamido]-5-oxo-7H-pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid

Common Name

English

OMAPATRILAT [JAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C247