Delving into the Latest Updates on Evatanepag with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Evatanepag (USAN/INN), Evatanepag Sodium

Target

EP2

Mechanism

EP2 agonists(Prostanoid EP2 receptor agonists)

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Tibial Fractures

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

Pfizer Inc.

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC25H28N2O5S

InChIKeyWOHRHWDYFNWPNG-UHFFFAOYSA-N

CAS Registry223488-57-1

ENSAYO ALEATORIZADO, CONTROLADO CON PLACEBO PARA EVALUAR LA EFICACIA, LA SEGURIDAD Y LA TOLERABILIDAD DE CP 533,536 EN PACIENTES CON FRACTURA CERRADA DE LA DIAFASIS TIBIALA RANDOMIZED, PLACEBO-CONTROLLED STUDY TO EVALUATE THE EFFICACY, SAFETY AND TOLERABILITY OF CP-533,536 IN SUBJECTS WITH CLOSED FRACTURE OF THE TIBIAL SHAFT

Start Date19 Nov 2008

Sponsor / Collaborator-

NCT00533377 / CompletedPhase 2

A Randomized, Placebo-Controlled Study To Evaluate The Efficacy, Safety And Tolerability Of CP-533,536 In Subjects With Closed Fracture Of The Tibial Shaft

The purpose of this study is to find out the good and bad effects of an investigational drug called CP-533,536 in patients with closed fracture of the tibial shaft undergoing internal fixation using reamed inter-locked IM nailing procedure

Start Date01 Jan 2008

Sponsor / Collaborator

Pfizer Inc.

100 Clinical Results associated with Evatanepag

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100 Translational Medicine associated with Evatanepag

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100 Patents (Medical) associated with Evatanepag

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9

Literatures (Medical) associated with Evatanepag

01 Jun 2020·Journal of Pharmacology and Experimental TherapeuticsQ3 · MEDICINE

Distribution and Function of Prostaglandin E₂Receptors in Mouse Uterus: Translational Value for Human Reproduction

Q3 · MEDICINE

Article

Author: Marshall, Kay M ; Fischer, Deborah P ; Lui, Sylvia ; Woodward, David F ; Farrar, Diane ; Sabar, Uzmah J ; Griffiths, Anna L ; O'Donovan, Peter J

Prostaglandin (PG) E analogs are used clinically to ripen the cervix and induce labor. However, selective receptor agonists may have potential to improve induction response rates or manage unwanted uterine hypercontractility in conditions such as dysmenorrhea and preterm labor. To characterize their therapeutic value, PGE₂ analogs were used to investigate the functional E-type prostanoid (EP) receptor population in isolated human uterus. Responsiveness in mouse tissues was also examined to validate its use as a preclinical model. Uterine samples were obtained from mice at dioestrus (n = 12), term gestation (n = 14), and labor (n = 12) and from the lower uterus of women undergoing hysterectomy (n = 12) or Caesarean section (n = 18). Vehicle and agonist effects were assessed using superfusion and immersion techniques. PGE₂ evoked predominant excitatory responses in mouse and relaxation in human tissues. Selective EP₄ agonists inhibited tissue activity in both nonpregnant species, while the EP₂ mimetic CP533536 also attenuated uterine contractions throughout gestation. The uterotonic effects of the EP_3/1 agonist sulprostone were more pronounced than the EP₁ agonist ONO-D1-004, corresponding to abundant EP₃ receptor expression in all samples. The contractile phenotype in mouse compared with human uteri may relate to regional differences as well as high expression of EP₃ receptor transcripts. Similarities in nonpregnant and gestational tissues across species suggest that EP₃ may represent a valuable translational drug target for preventing uterine hypercontractility by employing a selective antagonist. SIGNIFICANCE STATEMENT: This research validates the use of nonpregnant mice for preclinical drug discovery of uterine EP receptor targets. To determine the utility of novel drugs and delivery systems at term pregnancy and labor, pharmacological agents interacting with EP₃ receptors have clear translational value.

01 May 2010·IDrugs : the investigational drugs journal

American Society for Clinical Pharmacology and Therapeutics (ASCPT)-111th annual meeting. 17-20 March 2010, Atlanta, GA, USA.

Author: Veryard, Claire

The 111th Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics, held in Atlanta, included topics covering disclosures of new data in the field of pharmacokinetics and drug interactions. This conference report highlights selected presentations on pharmacokinetic studies of several investigational drugs, including evatanepag (Pfizer Inc), AEG-33773 (Aegera Therapeutics Inc), JNJ-16269110 (Johnson & Johnson Pharmaceutical Research & Development LLC), PF-3716539 (ViiV Healthcare), MK-0736 (Merck & Co Inc), a combination of Ginkgo biloba and cilostazol (Renexin SK Chemicals Co Ltd), PP-101 (Pacific Pharmaceuticals Co Ltd), ACT-178882 (Acetlion Ltd/Merck & Co Inc) and edoxaban (Daiichi Sankyo Co Ltd).

01 Apr 2009·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Discovery of CP-533536: An EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation

Q4 · MEDICINE

Article

Author: Paralkar, Vishwas M. ; Yu, Li ; Cameron, Kimberly O. ; Zawistoski, Michael P. ; Li, Mei ; Thompson, David D. ; Lefker, Bruce A. ; Wright, Ann S. ; Owen, Thomas A. ; Tjoa, Christina M. ; DeNinno, Shari L. ; Ke, Hua Z.

Sulfonamides, exemplified by 3a, were identified as highly selective EP(2) agonists. Lead optimization led to the identification of CP-533536, 7f, a potent and selective EP(2) agonist. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

100 Deals associated with Evatanepag

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External Link

KEGG	Wiki	ATC	Drug Bank
D09613	-	-	DB12022

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Tibial Fractures	Phase 2	US	Pfizer Inc.	01 Jan 2008
Tibial Fractures	Phase 2	RU	Pfizer Inc.	01 Jan 2008
Tibial Fractures	Phase 2	CA	Pfizer Inc.	01 Jan 2008
Tibial Fractures	Phase 2	IN	Pfizer Inc.	01 Jan 2008
Tibial Fractures	Phase 2	ES	Pfizer Inc.	01 Jan 2008
Tibial Fractures	Phase 2	HR	Pfizer Inc.	01 Jan 2008
Tibial Fractures	Phase 2	AU	Pfizer Inc.	01 Jan 2008
Tibial Fractures	Phase 2	BA	Pfizer Inc.	01 Jan 2008
Tibial Fractures	Phase 2	ZA	Pfizer Inc.	01 Jan 2008
Tibial Fractures	Phase 2	JP	Pfizer Inc.	01 Jan 2008