PF-05089771

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C18H12Cl2FN5O3S2
Molecular Weight	500.354
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

NC1=C(C=NN1)C2=CC(Cl)=CC=C2OC3=CC(F)=C(C=C3Cl)S(=O)(=O)NC4=CSC=N4

InChI

InChIKey=ZYSCOUXLBXGGIM-UHFFFAOYSA-N

InChI=1S/C18H12Cl2FN5O3S2/c19-9-1-2-14(10(3-9)11-6-24-25-18(11)22)29-15-5-13(21)16(4-12(15)20)31(27,28)26-17-7-30-8-23-17/h1-8,26H,(H3,22,24,25)

HIDE SMILES / InChI

Molecular Formula	C18H12Cl2FN5O3S2
Molecular Weight	500.354
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

Description

PF-05089771 is an oral administrated Nav1.7 channel inhibitor. PF-05089771 provided the best opportunity to explore Nav1.7 blockade for the treatment of acute or chronic pain conditions. PF-05089771 has completed Phase II clinical trials of third molar extraction and primary inherited erythromelalgia. The magnitude of efficacy of PF-05089771 in the randomized, placebo-controlled, double-blind clinical study in subjects with painful diabetic peripheral neuropathy was disappointing. Although there was a trend towards a reduction in pain and improvement in sleep rating in patients with painful DPN when compared to placebo treatment, this was not statistically significant.

Originator

Approval Year

Targets

Targets

Primary Target	Pharmacology	Potency
Sodium channel protein type IX alpha subunit 21	Blocker 537	0.011 µM [IC50]
Sodium channel protein type VIII alpha subunit 7	Blocker 537	0.16 µM [IC50]
Sodium channel protein type V alpha subunit 49	Blocker 537	25.0 µM [IC50]
Sodium channel protein type I alpha subunit 15	Blocker 537	0.85 µM [IC50]
Sodium channel protein type II alpha subunit 27	Blocker 537	0.11 µM [IC50]