mavatrep (JNJ-39439335) / J&J - LARVOL DELTA

TRPM3 mediates spontaneous pain and mechanical allodynia in a mouse model of chronic orofacial neuropathy. (PubMed, Cell Rep Med) - "Two structurally distinct TRPM3 antagonists, primidone and isosakuranetin, effectively reverse spontaneous pain and mechanical allodynia, whereas mavatrep, a potent TRPV1 antagonist, is without analgesic effect. These data indicate that TRPM3 is essential for ongoing pain and allodynia following trigeminal nerve injury, making it a potential target for treating trigeminally mediated neuropathic pain."

Journal • Preclinical • Neuralgia • Pain • TRPM3 • TRPV1

TRPV1 Receptor Modulators: Emerging Therapies for Neuropathic, Osteoarthritic, and Perioperative Pain. (PubMed, CNS Drugs) - "Promising pharmaceutical agonists for pain include low- and high-dose capsaicin formulations, resiniferatoxin, CNTX-4975, and vocacapsaicin. Potentially applicable antagonist drugs include NEO6860, Mavatrep, ACD-440, AJH-2947, DWP05195, and XEN-DO501. As our understanding of TRPV1 channels has continued to increase since the initial discovery, we are at last beginning to see some positive clinical developments for TRPV1 drugs in the realm of neuropathic, post-operative, musculoskeletal, and cancer pain."

Journal • Musculoskeletal Diseases • Musculoskeletal Pain • Oncology • Osteoarthritis • Pain

A study to investigate the safety, tolerability, and pharmacokinetics of JNJ-39439335 in healthy Japanese and Caucasian adult male participants (clinicaltrials.gov) - P1, N=86; Sponsor: Janssen Research & Development, LLC; Active, not recruiting -> Completed.

Trial completion • Pain

Bioavailability and Pharmacokinetics of TRPV1 Antagonist Mavatrep (JNJ-39439335) Tablet and Capsule Formulations in Healthy Men: Two Open-Label, Crossover, Single-Dose Phase 1 Studies. (PubMed, Clin Pharmacol Drug Dev) - "Mavatrep safety profiles were similar across formulations and under fasted and fed conditions. No new safety concerns were reported."

Clinical • Journal • P1 data • PK/PD data

Pharmacokinetics and Safety of Mavatrep (JNJ-39439335), a TRPV1 Antagonist in Healthy Japanese and Caucasian Men: A Double-Blind, Randomized, Placebo-Controlled, Sequential-Group Phase 1 Study. (PubMed, Clin Pharmacol Drug Dev) - "The most common adverse events observed were thermohypoesthesia, feeling cold, chills, and feeling hot. Mavatrep and its metabolites exhibited similar PK profiles after single ascending doses in healthy Japanese and caucasian men."

Clinical • Journal • P1 data • PK/PD data