Delving into the Latest Updates on FNDR-20081 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target-

Mechanism-

Therapeutic Areas

Infectious Diseases

Active Indication

Tuberculosis

Inactive Indication-

Originator Organization

Foundation For Neglected Disease Research

Active Organization

Foundation For Neglected Disease Research

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Author: Dusthackeer, Azger ; Loman, Nicholas J ; Nirmal, Christy Rosaline ; Eswaran, Sumesh ; Gangadharaiah, Shruthi Thimmalapura ; Krishnamurthy, Ramya Vadageri ; Kaur, Parvinder ; Naveenkumar, C N ; Narayanan, Shridhar ; Mondal, Rajesh ; Shandil, Radha Krishan ; Potluri, Vijay ; Shivarudraiah, Prasad ; Batt, Sarah M ; Besra, Gurdyal Singh ; Richardson, Emily J ; Ahuja, Vijay Kamal ; Mahizhaveni, Balasubramanian

FNDR-20081 [4-{4-[5-(4-Isopropyl-phenyl)- [1,2,4]oxadiazol-3-ylmethyl]-piperazin-1-yl}-7-pyridin-3-yl-quinoline] is a novel, first in class anti-tubercular pre-clinical candidate against sensitive and drug-resistant Mycobacterium tuberculosis (Mtb). In-vitro combination studies of FNDR-20081 with first- and second-line drugs exhibited no antagonism, suggesting its compatibility for developing new combination-regimens. FNDR-20081, which is non-toxic with no CYP3A4 liability, demonstrated exposure-dependent killing of replicating-Mtb, as well as the non-replicating-Mtb, and efficacy in a mouse model of infection. Whole genome sequencing (WGS) of FNDR-20081 resistant mutants revealed the identification of pleotropic targets: marR (Rv0678), a regulator of MmpL5, a transporter/efflux pump mechanism for drug resistance; and Rv3683, a putative metalloprotease potentially involved in peptidoglycan biosynthesis. In summary, FNDR-20081 is a promising first in class compound with the potential to form a new combination regimen for MDR-TB treatment.

100 Deals associated with FNDR-20081

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