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VYNE Therapeutics Announces Positive First-In-Human Pharmacokinetic and Hematology Data from Phase 1a Single and Multiple Ascending Dose Trial for Novel Pan-Bromodomain BET Inhibitor VYN201
No quantifiable VYN201 plasma concentrations above the assay lower limit of quantification supports “soft” drug approach for topical pan-BD BET inhibitor All
About this update from Vyne Therapeutics Inc.
[{"type":"text","content":"No quantifiable VYN201 plasma concentrations above the assay lower limit of quantification supports “soft” drug approach for topical pan-BD BET inhibitor All hematological parameters, including platelet counts, were within normal ranges, a finding which has not previously been observed with systemically administered pan-BD BET inhibitors Topline Phase 1b results in patients with nonsegmental vitiligo expected in mid-2023 BRIDGEWATER, N.J., March 30, 2023 (GLOBE NEWSWIRE) -- VYNE Therapeutics Inc. (Nasdaq: VYNE) (“VYNE” or the “Company”), a clinical-stage biopharmaceutical company developing proprietary, innovative and differentiated therapies for the treatment of immuno-inflammatory conditions, today announced positive first-in-human pharmacokinetic and hematology data from its Phase 1a single and multiple ascending dose trial for its investigational novel BET inhibitor, VYN201. In February 2023, the Company announced positive preliminary safety and tolerability data from the trial. The Phase 1a portion of the trial included comprehensive pharmacokinetic sampling to ascertain the exposure to topically-applied VYN201 from single and repeat treatment of VYN201 over five ascending dose cohorts. Results have shown that there were no quantifiable VYN201 plasma concentrations above the assay lower limit of quantification (0.25ng/ml). Inhibiting the functionality of the bromodomain 1 (BD1) subunit of BET proteins is believed to disrupt homeostatic gene regulation. This can lead to potential clinical safety concerns such as thrombocytopenia (low platelet count), a known dose-limiting adverse event for systemically administered pan-BD BET inhibitors.1 In the Phase 1a trial, there was no evidence of low or lower platelet counts at any timepoint for any dose cohort. The assay lower limit of quantification (LLOQ) of 0.25ng/ml is 720-fold below the free half maximal effective concentration (EC50) for VYN201 against the BD1 domain of the BET protein, BRD4. There was no effect on other assessed clinical hematological parameters. “These data, showing minimal systemic exposure of VYN201 with no effect on platelet counts, mark an important milestone in our development of VYN201 as a topically-administered pan-BD BET inhibitor,” said Dr. Iain Stuart, Chief Scientific Officer of VYNE. “These findings support our “soft” drug approach to treating pat...