Delving into the Latest Updates on CHMFL-KIT-033 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(E)‑N1‑(3-Fluorophenyl)‑N3‑(3-(2-(pyridin-2-yl)vinyl)‑1H‑indazol-6-yl)malonamide

Target

c-Kit

Mechanism

c-Kit inhibitors(Stem cell growth factor receptor inhibitors)

Therapeutic Areas

NeoplasmsDigestive System DisordersSkin and Musculoskeletal Diseases+ [1]

Active Indication

Gastrointestinal Stromal Tumors

Inactive Indication-

Originator Organization

Hefei Institutes of Physical Science

Active Organization

Hefei Institutes of Physical Science

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Oxytocin is known to be implicated in a variety of functions, such as learning, stress, anxiety, feeding, and pain perception. Oxytocin is also important for social memory and attachment, human bonding, sexual and maternal behaviour, and aggression. Human disorders characterized by aberrant social interactions, such as autism and schizophrenia, may also involve abnormal oxytocin levels. GSK712043, GSK711320, and GSK664004, three antagonists exhibiting subnanomolar affinity for the human oxytocin receptor (hOTR) and high selectivity over vasopressin receptors were successfully labelled with carbon‐11 with suitable yields (0.5‐1GBq @EOS), high molar activity (275‐700 GBq/μmol), and radiochemical purities. The in vivo regional uptake of these radiotracers was determined in porcine brain. [11C]GSK711320 baseline scan showed no significant brain uptake, and limited initial uptake was observed following administration of [11C]GSK712043 or [11C]GSK664004. The [11C]GSK712043 and [11C]GSK664004 kinetics were slow and peaked at around 2%ID/L at 90 minutes post‐injection. For both tracers, the distribution of activity was homogeneous throughout the brain. All the tracers showed high uptake in the pituitary gland, especially [11C]GSK711320; however, its uptake could not be blocked by pretreatment with the known OTR antagonist, L368,899. In vivo evaluation of these candidates demonstrated that they are not suitable as central OTR PET imaging agents.

100 Deals associated with CHMFL-KIT-033

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