Pasithea Therapeutics to Present Preclinical Data on PAS-004's Efficacy Against NRAS Cancer at 2024 ASCO

Pasithea Therapeutics Corp., a biotech company in the clinical stage, has announced promising preclinical results of its drug PAS-004. This next-generation macrocyclic MEK inhibitor is being developed for treating neurofibromatosis type 1 (NF1) and other cancers. The data revealed that PAS-004 strongly inhibits NRAS mutant cancer cell lines with IC50 values between 0.024 and 0.306 µM. Notably, PAS-004 achieved over 50% growth inhibition in more cell lines compared to binimetinib and selumetinib. Its inhibitory effect was comparable to trametinib across five cell lines, but unlike trametinib, PAS-004 did not reach a plateau.

These significant findings will be presented at the American Society of Clinical Oncology (ASCO) Annual Meeting on June 1, 2024, in Chicago. During this event, attendees will be able to see a poster detailing the efficacy of PAS-004 in both in vitro and xenograft tumor models. Dr. Tiago Reis Marques, CEO of Pasithea, expressed excitement about the enhanced potency of PAS-004 relative to approved agents, noting its potential for less frequent dosing and improved patient compliance. He emphasized that PAS-004 strikes a balance between pharmacokinetics (PK), pharmacodynamics (PD), and tolerability, making it a promising candidate for NF1 and various cancers. The company anticipates initial results from their Phase 1 clinical trial soon.

PAS-004 is groundbreaking as the first macrocyclic MEK inhibitor to enter human clinical trials. Its extended half-life could lead to higher compliance rates and improved efficacy in treating NF1. Macrocycles typically show stronger binding, better solubility, and longer half-life compared to acyclic molecules, offering enhanced selectivity and fewer off-target effects.

The poster presentation, entitled "PAS-004: A novel macrocyclic MEK inhibitor to inhibit cancer cell growth in vitro and tumor growth in mouse xenograft studies," will be led by Dr. Graeme Currie. The session is part of the ASCO Annual Meeting's Developmental Therapeutics segment focused on molecularly targeted agents and tumor biology.

PAS-004 functions as an allosteric inhibitor of MEK 1/2 in the MAPK signaling pathway, crucial for cell proliferation, differentiation, and survival. Abnormal activation of this pathway contributes to tumor formation and progression. Current FDA-approved MEK inhibitors, used for various cancers and NF1, have notable toxicities. PAS-004, being macrocyclic, may offer better pharmacokinetics and safety. Its rigid structure allows better binding to target receptors, potentially giving a longer half-life and a better therapeutic window.

Pasithea has demonstrated PAS-004’s potency and safety in preclinical studies, suggesting the drug may deliver more durable responses and better dosing schedules. PAS-004 has undergone extensive preclinical testing, including animal toxicology studies, and received orphan-drug designation from the FDA for NF1 treatment.

Pasithea Therapeutics Corp. is dedicated to developing innovative treatments for central nervous system disorders and RASopathies. With a team of experts in neuroscience, translational medicine, and drug development, the company is advancing new molecular entities for treating neurological disorders, including NF1, solid tumors, and amyotrophic lateral sclerosis (ALS).

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