PF-05105679

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C26H21FN2O3
Molecular Weight	428.4549
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

C[C@@H](N(CC1=CC(=CC=C1)C(O)=O)C(=O)C2=CC3=C(C=CC=C3)N=C2)C4=CC=C(F)C=C4

InChI

InChIKey=BXNMZRPTQFVRFA-QGZVFWFLSA-N

InChI=1S/C26H21FN2O3/c1-17(19-9-11-23(27)12-10-19)29(16-18-5-4-7-21(13-18)26(31)32)25(30)22-14-20-6-2-3-8-24(20)28-15-22/h2-15,17H,16H2,1H3,(H,31,32)/t17-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C26H21FN2O3
Molecular Weight	428.4549
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

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

Approval Year

Targets

Targets

Primary Target	Pharmacology	Condition	Potency
Transient receptor potential cation channel subfamily M member 8 18	Inhibitor 8,504		103.0 nM [IC50]

Substance Class	Chemical
Record UNII	F2B10OFV7Y
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PF-05105679

Common Name

English

PF 5105679

Preferred Name

English

BENZOIC ACID, 3-((((1R)-1-(4-FLUOROPHENYL)ETHYL)(3-QUINOLINYLCARBONYL)AMINO)METHYL)-

Systematic Name

English

3-((((1R)-1-(4-FLUOROPHENYL)ETHYL)(3-QUINOLINYLCARBONYL)AMINO)METHYL)-BENZOIC ACID

Systematic Name

English

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Code System

Code

Type

Description

CAS

1398583-31-7

PRIMARY

EPA CompTox

DTXSID301336742

PRIMARY

DRUG BANK

DB15450

PRIMARY

FDA UNII

F2B10OFV7Y

PRIMARY

PUBCHEM

60195662

PRIMARY

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Related Record

Type

Details


					F2B10OFV7Y

PF-05105679

ACTIVE MOIETY

Comments:

The transient receptor potential (TRP) family of ion channels comprises nonselective cation channels that respond to a wide range of chemical and thermal stimuli. TRPM8, a member of the melastatin subfamily, is activated by cold temperatures (<28 C), and antagonists of this channel have the potential to treat cold induced allodynia and hyperalgesia. However, TRPM8 has also been implicated in mammalian thermoregulation and antagonists have the potential to induce hypothermia in patients. We report herein the identification and optimization of a series of TRPM8 antagonists that ultimately led to the discovery of PF-05105679. The clinical finding with this compound will be discussed, including both efficacy and its ability to affect thermoregulation processes in humans.


					F2B10OFV7Y

PF-05105679

ACTIVE MOIETY

Comments:

Originator: Pfizer; Class: Analgesic; Mechanism of Action: TRPM8 protein inhibitor; Orphan Drug Status: No; On Fast track: No; New Molecular Entity: Yes; Highest Development Phase: No development reported for Pain; Most Recent Events: 30 Sep 2011 Pfizer completes a phase I trial in Healthy volunteers in Belgium (NCT01393652), 23 May 2011 Phase-I clinical trials in Pain in Belgium (unspecified route)


					F2B10OFV7Y

PF-05105679

ACTIVE MOIETY

Comments:

Official Title: A Phase I, Randomized, Placebo-Controlled, Dose Escalating Cross Over Study To Evaluate The Safety, Toleration, Pharmacokinetics And Pharmacodynamics Of PF-05105679 Under Fasted Conditions In Healthy Volunteers Purpose: This is a two part study. The purpose of the first part (Part A) is the evaluation of the pharmacokinetics, safety and tolerability after single ascending dose of PF-05105679. The second part (Part B) of this study will focus on the exploratory pharmacodynamics of PF-05105679 using pharmacodynamics markers (cold detection) in healthy volunteers. The doses selected in Part B will have been administered previously in the Part A of the study.


					F2B10OFV7Y

PF-05105679

ACTIVE MOIETY

Comments:

Drugs: Oxycodone, PF 5105679; Indication: Pain; Focus: Adverse reactions, Pharmacodynamics, Pharmacokinetics; Acronyms: SINGLE DOSE; Most Recent Events: 30 Sep 2011 Status changed from recruiting to completed as reported by ClinicalTrials.gov., 15 Jul 2011 New trial record

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