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PLS-3
- Development stage
- Preclinical
- Lead developer
- Primetime
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
PLS-3 is a small molecule agonist of the thyrotropin-releasing hormone receptor (TRHR) being developed by Primetime Life Sciences for the treatment of cancer-related fatigue (CRF). TRHR is a G protein-coupled receptor widely distributed throughout the central nervous system (CNS) and peripheral tissues. Activation of TRHR by thyrotropin-releasing hormone (TRH) or its analogs is known to exert arousing, analeptic, and mood-elevating effects. PLS-3 is designed as a "super-agonist" with significantly higher intrinsic efficacy and potency than native TRH and existing analogs such as taltirelin. The compound is engineered to be metabolically stable and blood-brain barrier permeable, addressing the pharmacokinetic limitations of earlier TRH-based therapies. PLS-3 has demonstrated efficacy in preclinical mouse models of fatigue and is being advanced through a Cooperative Research and Development Agreement (CRADA) with the NIDDK/NIH.
- Other names
- TRHR agonist
02
Targets
TRHR (Thyrotropin-releasing hormone receptor)
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