NICARAVEN, (+)-

Investigational

Details

Stereochemistry	UNKNOWN
Molecular Formula	C15H16N4O2
Molecular Weight	284.3131
Optical Activity	( + )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC(CNC(=O)C1=CC=CN=C1)NC(=O)C2=CN=CC=C2

InChI

InChIKey=KTXBOOWDLPUROC-UHFFFAOYSA-N

InChI=1S/C15H16N4O2/c1-11(19-15(21)13-5-3-7-17-10-13)8-18-14(20)12-4-2-6-16-9-12/h2-7,9-11H,8H2,1H3,(H,18,20)(H,19,21)

HIDE SMILES / InChI

Molecular Formula	C15H16N4O2
Molecular Weight	284.3131
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description

Nicaraven is a hydroxyl radical scavenger with antivasospastic and neuroprotective effects. Chugai (the Japanese subsidiary of Roche) is developing nicaraven (Antevas), a water-soluble antioxidant, for the potential treatment of disorders caused by acute cerebrovascular diseases. A registration application was filed in April 1995, and in April 2002, nicaraven was still awaiting registration in Japan. By August 2002, Chugai had filed an NDA in Japan for the additional indication of subarachnoidal bleeding.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
PARP 1, 2 and 3 7	Inhibitor 8,504		1.5 mM [IC50]
Oxidative Stress 162	Inhibitor 8,504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Subarachnoid hemorrhage 8	Primary		Not Provided 511	Unknown

PubMed

Show entries

Title	Date	PubMed
		28326999
The potential benefits of nicaraven to protect against radiation-induced injury in hematopoietic stem/progenitor cells with relative low dose exposures.	2014 Sep 26	25173934
Nicaraven, a Potential Radioprotective Agent, has Very Limited Effects on the Survival of Cancer Cells and the Growth of Established Tumors.	2017 Feb 22	28225650

Showing 1 to 3 of 3 entries

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Patents

Sample Use Guides

In Vivo Use Guide

4 g nicaraven infused intravenously for 6-8 hours once a day

Route of Administration: Intravenous

In Vitro Use Guide

The antiplatelet activities in vitro of nicaraven were examined. The concentrations of nicaraven tested were 3.50 x 10(-5) mol/L, 1.75 x 10(-4) mol/L, 3.50 x 10(-4) mol/L, and 1.75 x 10(-3) mol/L, respectively. The maximum aggregation rate induced by adenosine diphosphate (ADP) was significantly inhibited by nicaraven at concentration ranges of 3.50 x 10(-4) mol/L or higher in the healthy volunteer platelets. The maximum aggregation rate induced by collagen was significantly inhibited by 1.75 x 10(-3) mol/L of nicaraven. Using platelets from patients with cerebral thrombosis, the maximum aggregation rate induced by ADP was significantly inhibited by 1.75 x 10(-3) mol/L of nicaraven. Furthermore, the maximum aggregation rate induced by collagen were significantly reduced by 1.75 x 10(-3) mol/L of nicaraven.