PEMRAMETOSTAT

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C24H32N6O3
Molecular Weight	452.5493
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(=O)N1CCC(CC1)NC2=CC(=NC=N2)C(=O)NC[C@H](O)CN3CCC4=CC=CC=C4C3

InChI

InChIKey=JLCCNYVTIWRPIZ-NRFANRHFSA-N

InChI=1S/C24H32N6O3/c1-17(31)30-10-7-20(8-11-30)28-23-12-22(26-16-27-23)24(33)25-13-21(32)15-29-9-6-18-4-2-3-5-19(18)14-29/h2-5,12,16,20-21,32H,6-11,13-15H2,1H3,(H,25,33)(H,26,27,28)/t21-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C24H32N6O3
Molecular Weight	452.5493
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Protein arginine N-methyltransferase 5 2 Target ID: CHEMBL1795116 Sources: https://worldwide.espacenet.com/publicationDetails/biblio?DB=EPODOC&II=0&ND=3&adjacent=true&locale=en_EP&FT=D&date=20140626&CC=WO&NR=2014100719A2&KC=A2	Inhibitor 8504

C_max

Value	Dose	Analyte	Population
1322.8 ng/mL CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
960.4 ng/mL CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1125.4 ng/mL CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
889.7 ng/mL CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
7128.4358 ng × h/mL CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6572.8527 ng × h/mL CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9202.5641 ng × h/mL CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6397.084 ng × h/mL CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
5.0755 h CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.7688 h CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.2694 h CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.8437 h CLINICAL TRIAL https://clinicaltrials.gov/study/NCT03614728?term=GSK-3326595&rank=1&tab=results	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	EPZ-015938 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Overview

CYP3A4	CYP2C9	CYP2D6	hERG

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer

Substance Class	Chemical Created by `admin` on `Mon Mar 31 23:17:38 GMT 2025` Edited by `admin` on `Mon Mar 31 23:17:38 GMT 2025`
Record UNII	VXT8SZ6875
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PEMRAMETOSTAT

Official Name

English

4-PYRIMIDINECARBOXAMIDE, 6-((1-ACETYL-4-PIPERIDINYL)AMINO)-N-((2S)-3-(3,4-DIHYDRO-2(1H)-ISOQUINOLINYL)-2-HYDROXYPROPYL)-

Preferred Name

English

GSK-3326595

Common Name

English

pemrametostat [INN]

Common Name

English

GSK-3326595A

Code

English

EPZ015938

Code

English

EPZ-015938

Code

English

PROTEIN ARGININE METHYLTRANSFERASE 5 INHIBITOR GSK3326595

Common Name

English

6-((1-ACETYL-4-PIPERIDINYL)AMINO)-N-((2S)-3-(3,4-DIHYDRO-2(1H)-ISOQUINOLINYL)-2-HYDROXYPROPYL)-4-PYRIMIDINECARBOXAMIDE

Systematic Name

English

Pemrametostat [WHO-DD]

Common Name

English

GSK3326595

Code

English

Code System Code Type Description

CAS

1616392-22-3