ARV-102 / Arvinas - LARVOL DELTA

Arvinas Presents First-in-Human Data for Investigational Oral PROTAC ARV-102 Demonstrating Blood-Brain Barrier Penetration, and Central and Peripheral LRRK2 Degradation (GlobeNewswire) - P1 | N=47 | 2024-516888-84-00 | Sponsor: Arvinas Operations Inc. | "Results...were shared in a presentation at the 2025 International Conference on Alzheimer’s and Parkinson’s Diseases (AD/PD 2025)...At a single oral dose of at least 60 mg, and once daily repeated oral doses of at least 20 mg, ARV-102 achieved greater than 50% LRRK2 reduction in the CSF and greater than 90% LRRK2 reduction in the peripheral blood mononuclear cells (PBMCs), indicating substantial central and peripheral LRRK2 protein degradation...Of the 47 volunteers across all SAD dose levels, the primary treatment related adverse events were headache and fatigue...ARV-102 exhibited median maximum concentration (Tmax) 6 hours after oral administration...ARV-102 at single doses of greater than or equal to 30 mg induced greater than 50% decreases in peripheral phospho-Rab10T73, a LRRK2 substrate and biomarker for downstream LRRK2 activity; data for this endpoint in the MAD cohort is pending."

P1 data • Parkinson's Disease

Anticipated Upcoming Milestones and Expectations (GlobeNewswire) - "ARV-102: Oral PROTAC LRRK2 degrader: Present final data from the SAD/MAD cohorts of the Phase 1 clinical trial in healthy volunteers (2H 2025); Continue enrollment and present initial data from the SAD cohort of the ongoing Phase 1 clinical trial in patients with Parkinson’s disease (2H 2025); Initiate the MAD cohort of the Phase 1 clinical trial in patients with Parkinson’s disease (2H 2025)."

P1 data • Trial status • Parkinson's Disease

Investigational therapy ARV-102 now in Parkinson’s trial (Parkinson's News Today) - "Arvinas has begun a Phase 1 clinical trial to test its investigational therapy ARV-102 in people with Parkinson’s disease, with Phase 1 data in healthy adults showing it was safe and worked as expected....The study involving people with Parkinson’s (EUCT 2024-516888-84-00) was initiated at the end of 2024 and is still recruiting adults at a site in the Netherlands. Arvinas expects to present some data this year."

P1 data • Trial status • Parkinson's Disease

FIRST-IN-HUMAN STUDY TO ASSESS THE SAFETY, PHARMACOKINETICS, AND PHARMACODYNAMICS OF ARV-102, A PROTAC LRRK2 DEGRADER, IN HEALTHY MALES (ADPD 2025) - "Conclusions At single doses of 10–200 mg, ARV-102 was orally bioavailable, well tolerated, and achieved substantial peripheral LRRK2 protein degradation with evidence of CNS distribution and target engagement. This study supports continued investigation of ARV-102 in neurodegenerative diseases associated with LRRK2 dysfunction."

Clinical • P1 data • PK/PD data • CNS Disorders • Targeted Protein Degradation • LRRK2 • RAB10

Arvinas Announces Oral Presentation at 2025 International Conference on Alzheimer’s & Parkinson’s Diseases (GlobeNewswire) - "Arvinas...today announced that data from the first-in-human study evaluating single-ascending and multiple-ascending doses in healthy volunteers of ARV-102 will be presented at the International Conference on Alzheimer’s and Parkinson’s Diseases (AD/PD), April 1-5, 2025 in Vienna, Austria."

P1 data • Alzheimer's Disease • Parkinson's Disease

Arvinas Reports Fourth Quarter and Full Year 2024 Financial Results and Provides Corporate Update (GlobeNewswire) - "ARV-102: Oral PROTAC LRRK2 degrader: Present SAD data from the ongoing Phase 1 clinical trial in healthy volunteers in an oral session at the Alzheimer’s Disease/Parkinson’s Disease (AD/PD) conference in Vienna, Austria (April 1-4, 2025) demonstrating: Bioavailability and brain penetration with dose dependent exposure in cerebral spinal fluid (CSF); Degradation of LRRK2 in the periphery and CSF of healthy volunteers. Complete enrollment and present initial data from the ongoing SAD Phase 1 clinical trial in patients with PD in 2025; initiate MAD cohort in patients with PD in 2025."

P1 data • Alzheimer's Disease • Parkinson's Disease