Arvinas presents data from two Phase 1 trials for ARV-102

Arvinas (ARVN) announced positive pharmacokinetic, pharmacodynamic, and biomarker data from two Phase 1 clinical trials evaluating ARV-102, an oral, brain-penetrant investigational PROTAC degrader of leucine-rich repeat kinase 2. The company presented data from two trials: ARV-102-101, a first-in-human trial of ARV-102 in healthy volunteers, and ARV-102-103, a trial in patients with Parkinson’s disease. Key findings include: Data from a Phase 1 Single Ascending Dose and Multiple Ascending Dose Trial in Healthy Volunteers: Safety: ARV-102 was generally well tolerated at single doses up to 200 mg and multiple daily doses up to 80 mg, with no discontinuations due to adverse events or serious adverse events observed in the study population. Pharmacokinetics: ARV-102 exposure increased in a dose-dependent manner in plasma and CSF, the latter indicating brain penetration. Pharmacodynamics: Repeated daily doses greater than or equal to20 mg resulted in greater than90% reductions of LRRK2 protein in peripheral blood mononuclear cells and greater than50% reductions in CSF. Interim Single Ascending Dose Data from a Phase 1 Trial in Patients with Parkinson’s Disease and CSF Proteomic Data from a Phase 1 Trial in Healthy Volunteers: Safety: The Phase 1 trial in patients with Parkinson’s disease included 15 patients treated with ARV-102 and 4 patients treated with placebo. In the trial, single doses of ARV-102 were well tolerated with only mild treatment-related AEs including headache, diarrhea, and nausea; no SAEs occurred. Pharmacokinetics: In patients with Parkinson’s disease, ARV-102 exposure increased in a dose-dependent manner in both plasma and CSF, the latter indicating brain penetration. Pharmacodynamics: In patients with Parkinson’s disease, treatment with ARV-102 resulted in median PBMC LRRK2 protein reductions of 86% with the 50 mg dose and 97% with the 200 mg dose.