JNJ-26483327

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H25BrN4O2
Molecular Weight	457.364
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

COC1=CC2=NC=NC3=C2C=C1OCCCCCN(C)CC4=CC=C(Br)C=C4N3

InChI

InChIKey=JXDYOSVKVSQGJM-UHFFFAOYSA-N

InChI=1S/C22H25BrN4O2/c1-27-8-4-3-5-9-29-21-11-17-19(12-20(21)28-2)24-14-25-22(17)26-18-10-16(23)7-6-15(18)13-27/h6-7,10-12,14H,3-5,8-9,13H2,1-2H3,(H,24,25,26)

HIDE SMILES / InChI

Molecular Formula	C22H25BrN4O2
Molecular Weight	457.364
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Approval Year

Substance Class	Chemical
Record UNII	16720VER1H
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

JNJ-26483327

Code

English

4,6-ETHENOPYRIMIDO(4,5-B)(6,1,12)BENZOXADIAZACYCLOPENTADECINE, 17-BROMO-1,8,9,10,11,12,13,14-OCTAHYDRO-20-METHOXY-13-METHYL-

Systematic Name

English

JNJ 26483327 [WHO-DD]

Common Name

English

17-BROMO-1,8,9,10,11,12,13,14-OCTAHYDRO-20-METHOXY-13-METHYL-4,6-ETHENOPYRIMIDO(4,5-B)(6,1,12)BENZOXADIAZACYCLOPENTADECINE

Systematic Name

English

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Code System

Code

Type

Description

ChEMBL

CHEMBL3545133

PRIMARY

CAS

807640-87-5

PRIMARY

MANUFACTURER PRODUCT INFORMATION

JNJ-26483327

PRIMARY

CLINICAL_TRIALS.GOV

JNJ-26483327

PRIMARY

Official Title: An Open-label, Phase I Study to Determine the Safety and Pharmacokinetics of JNJ-26483327, a Multi-targeted Kinase Inhibitor, Administered to Subjects With Advanced Stage and/or Refractory Solid MalignanciesDetailed Description:JNJ-26483327, a multi-targeted reversible kinase inhibitor, is a new drug in development for treatment of cancer. This study will test the safety (the effect on the body) of JNJ-26483327 and the highest dose of JNJ-26483327 that patients with advanced cancer can tolerate will be determined. Antitumor activity of JNJ-26481585 will be evaluated.

PUBCHEM

11952856

PRIMARY

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Related Record

Type

Details


					16720VER1H

JNJ-26483327

ACTIVE MOIETY

Comments:

RESULTS: JNJ-26483327 was well tolerated in doses up to 1500 mg BID, with target-inhibition-related toxicity such as diarrhoea and skin rash, and other common reported toxicities being nausea, vomiting, anorexia and fatigue. At 2100 mg, two episodes of dose-limiting toxicity were observed, consisting of grade 3 anorexia and a combination of grade 3 anorexia and fatigue, respectively. Pharmacokinetics were dose proportional up to 1500 mg in which plasma levels were obtained showing anti-tumour activity in xenograft mouse models. Pharmacodynamic analysis did not show a substantial effect on expression of Ki-67, p27(kip1), phosphorylated mitogen-activated protein kinase, phosphorylated Akt and EGFR, and serum levels of sVEGFR-2, VEGF-C and VEGF-D remained unchanged. Stable disease was noted in six patients (32%).


					16720VER1H

JNJ-26483327

ACTIVE MOIETY

Comments:

Class: Antineoplastic, Macrocyclic compound, Small molecule; Mechanism of Action: Epidermal growth factor receptor antagonist, Protein tyrosine kinase inhibitor, Src-Family kinase inhibitor, Vascular endothelial growth factor receptor 3 antagonist; Highest Development Phase: Phase I for Solid tumours; Most Recent Events: 14 Oct 2011 JNJ 26483327 licensed to BeiGene worldwide, 19 Nov 2009 Interim adverse events, pharmacokinetic and efficacy data from a phase I trial in Solid tumours presented at the 21st AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics (AACR-NCI-EORTC-2009), 31 Aug 2006 Phase I clinical trials in advanced and/or refractory solid tumours in the US (PO)

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