ADRIFORANT

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C13H22N6
Molecular Weight	262.354
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN[C@@H]1CCN(C1)C2=CC(NCC3CC3)=NC(N)=N2

InChI

InChIKey=ISBHYKVAFKTATD-SNVBAGLBSA-N

InChI=1S/C13H22N6/c1-15-10-4-5-19(8-10)12-6-11(17-13(14)18-12)16-7-9-2-3-9/h6,9-10,15H,2-5,7-8H2,1H3,(H3,14,16,17,18)/t10-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C13H22N6
Molecular Weight	262.354
Charge	0
Count

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23558237 | https://www.ncbi.nlm.nih.gov/pubmed/23276980 | https://adisinsight.springer.com/drugs/800027924 | https://www.ncbi.nlm.nih.gov/pubmed/21920751

PF-03893787 is potent and selective histamine H4 receptor (H4R) antagonist. It has comparable binding affinity to the human histamine H3 receptor. PF-03893787 was found to have significant affinity for the hERG channel. Novartis initiates a phase II extension trial in Atopic dermatitis. Studies exploring the utility of PF-3893787 in patients would be reported in due course, being the potential indications of asthma, pruritus, inflammatory skin diseases and pain, among others.

Originator

Approval Year

PubMed

Title	Date	PubMed
Molecularly targeted therapies for asthma: Current development, challenges and potential clinical translation.	2016-10	27453494
A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.	2013-05-01	23558237
Is the H4 receptor a new drug target for allergies and asthma?	2013-01-01	23276980
Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.	2011-11-01	21920751

Sample Use Guides

In Vivo Use Guide

5, 15, 50 mg, QD for 14 days

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Mon Mar 31 23:12:42 GMT 2025` Edited by `admin` on `Mon Mar 31 23:12:42 GMT 2025`
Record UNII	D65H9YE9VU
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ADRIFORANT

Official Name

English

PF-03893787

Preferred Name

English

ZPL389-NX

Code

English

NVP-ZPL389-NX

Code

English

N4-(Cyclopropylmethyl)-6-[(3R)-3-(methylamino)pyrrolidin-1-yl]pyrimidine-2,4-diamine

Systematic Name

English

ZPL-389-NX

Code

English

PF-3893787

Code

English

Adriforant [WHO-DD]

Common Name

English

ADRIFORANT [USAN]

Common Name

English

adriforant [INN]

Common Name

English

2,4-PYRIMIDINEDIAMINE, N4-(CYCLOPROPYLMETHYL)-6-((3R)-3-(METHYLAMINO)-1-PYRROLIDINYL)-

Systematic Name

English

ZPL-3893787

Code

English

ZPL-389

Code

English

Code System Code Type Description

EVMPD

SUB194074