Delving into the Latest Updates on CP-0840 with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Target

bradykinin receptor x μ opioid receptor

Action

antagonists, agonists

Mechanism

bradykinin receptor antagonists(Bradykinin receptors antagonists), μ opioid receptor agonists(Mu opioid receptor agonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication-

Inactive Indication

InflammationPain

Originator Organization

Cortech, Inc.

Active Organization-

Inactive Organization

Cortech, Inc.

License Organization-

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC87H130N18O17S

InChIKeyGNTGLHNCRADSMA-RLTWNPMHSA-N

CAS Registry186127-95-7

Author: Val S. Goodfellow ; John S. Zuzack ; Lyle W. Spruce ; Michael Burkard ; Steven W. Jones ; Mary D. Francis ; Anna Pilyavskaya ; Sherman E. Ross ; Virginia E. Beckey ; Eric T. Whalley ; Maciej Wieczorek ; Manoj V. Marathe ; Albert Gyorkos ; Lajos Gera ; Timothy D. Fitzpatrick ; John M. Stewart ; William M. Selig

The determination of the relationship between ligand affinity and bioactivity is important for the understanding of receptor function in biological systems and for drug development. Several physiological and pathophysiological functions of bradykinin (BK) are mediated via the B2 receptor. In this study, we have examined the relationship between B2 receptor (soluble and membrane-bound) binding of BK peptidic antagonists, inhibition of calcium signalling at a cellular level, and in vitro inhibition of ileum contraction. Only human systems were employed in the experiments. Good correlations between the studied activities of BK antagonists were observed for a variety of different peptidic structures. The correlation coefficients (r) were in the range of 0.905 to 0.955. In addition, we analyzed the effect of the C-terminal Arg9 removal from BK and its analogs on B2 receptor binding. The ratios of binding constants (Ki(+Arg)/Ki(-Arg)) for the Arg9 containing compounds and the corresponding des-Arg9 analogs varied from about 10 to 250,000. These ratios strongly depend on the chemical structures of the compounds. The highest ratios were observed for two natural agonist pairs, BK/des-Arg9-BK and Lys0-BK/des-Arg9-Lys0-BK.

100 Deals associated with CP-0840

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Inflammation	Discovery	United States	Cortech, Inc.	-
Pain	Discovery	United States	Cortech, Inc.	-

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Clinical Result

Indication

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Approval

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Biosimilar

Competitive landscape of biosimilars in different countries/locations. Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3.

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