PAH therapy with a TRPC3/6 inhibitor exahibiting good pharmacokinetics

It has been synthesized a stable and specific inhibitor for TRPC3/6 which shows a therapeutic effect on mouse model of Pulmonary Arterial Hypertension (PAH)

Advantages

  • It has confirmed excellent chemical, physical stability, pharmacokinetics and low toxicity in rodent study
  • It has also been observed the therapeutic efficacy for fibrosis, that is implied the pathological relation to TRPC3/6 expression

Background and Technology

TRPC6 and TRPC3 are receptor-activated nonselective cation channels that belong to a family of canonical transient receptor potential channels. TRPC3/6 are involved in many physiological or pathological processes, such as synaptic formation, kidney function, wound healing and cardiac hypertrophy induction.  However, many inhibitors for TRPC3 and TRPC6 are developed as therapeutic agents by pharmaceutical companies, most of trials seems to be failed.  One of a difficult on developing TRPC3/6 inhibitors is poor pharmacokinetics of these compounds.

We success to develop specific inhibitors L-862 for TRPC3/6 that shows good stability, safety profile and pharmacokinetics.  We confirmed therapeutic effect on rat PAH model induced by MCT (monocrotaline).  We also have obtained efficacy data for fibrosis.

Data

  •  L862 inhibited selectively TRPC3/6 rather than other TRP channels (C1, C2, C5, C7, A1, V1, V6, M2, M8) in vitro
  • MCT induced elevation of right ventricular systolic pressure (RSVP) in rat was suppressed by administration of L862
  • L-862 was exhibited good oral absorbability and blood kinetics in PK and TK study in rat
  • Sufficient safety data are observed in single and repeated oral toxicity study, AMES test and in vitro cardio-toxicity test

Patent

Patent No. WO2019/208812

Researcher

Ryu Nagata (Osaka University)

Expectations

We expect the collaboration with the companies or the capitalization of investors to develop L-862 for a preclinical and later stage.

Under CDA, I can disclose the detailed information about PK and the toxicology profile.   In addition, we can provide compounds synthesized for patent license evaluation under a technology evaluation agreement or MTA, both of which require a fee.

Product No:WL-02528a

Medicine

Updated
Published

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