PM534 / PharmaMar - LARVOL DELTA

PM534, a Novel Colchicine‑Site Tubulin Inhibitor with Broad‑Spectrum and Resistance‑Overcoming Antitumor Activity. (PubMed, Mol Cancer Ther) - P1 | "Collectively, these findings highlight PM534 as a promising antitumor agent with potent activity against diverse and treatment-resistant malignancies. A Phase I clinical trial (NCT05835609) is underway to assess the therapeutic potential of PM534 in patients with advanced solid tumors."

Journal • Genito-urinary Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Solid Tumor • Triple Negative Breast Cancer

PM534 Administered Intravenously to Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=30 | Recruiting | Sponsor: PharmaMar | Trial completion date: Mar 2025 ➔ Oct 2026 | Trial primary completion date: Mar 2025 ➔ Oct 2026

Trial completion date • Trial primary completion date • Breast Cancer • Prostate Cancer • Solid Tumor

PharmaMar presents eleven scientific publications at the Annual Meeting of the American Association for Cancer Research (AACR) (Pharmamar Press Release) - "On this occasion, the Company is presenting eleven new studies with results on the activity of its compounds: lurbinectedin (Zepzelca), ecubectedin, PM54, PM534, and trabectedin (Yondelis)....The main conclusions from the presented studies highlight the potential of two novel transcription inhibitors, PM54 and ecubectedin as innovative antitumor agents. Ecubectedin has demonstrated encouraging antitumor efficacy in both gastric and neuroendocrine-prostate cancer models. In collaboration with KU Leuven University (Belgium), data also confirm promising antitumor activity of both ecubectedin and PM54 in representative models of soft tissue sarcomas (STS)....Additionally, data on PM534 are being presented. PM534 is a novel tubulin-targeting agent, that may bypass the most common resistance mechanisms, limiting the effectiveness of standard microtubule-binding drugs."

Clinical data • Preclinical • Gastric Cancer • Neuroendocrine Carcinoma • Prostate Cancer • Soft Tissue Sarcoma • Solid Tumor

Overcoming resistance to tubulin-targeting drugs with PM534: an innovative microtubule-targeting compound (AACR 2025) - "PM534's efficacy surpassed paclitaxel in these resistant models, as its activity remained unaffected by Pgp overexpression or β-III tubulin presence—both common resistance mechanisms that limit other tubulin-targeting drugs. In conclusion, PM534 demonstrates potent antitumor activity in drug-resistant cancer models, effectively bypassing Pgp-mediated efflux and β-III tubulin-related resistance. These findings support PM534's potential as a promising therapeutic candidate capable of overcoming the limitations of current tubulin-targeting agents in oncology."

Oncology • ABCB1

From Sea Sponge to Clinical Trials: Starting the Journey of the Novel Compound PM742. (PubMed, Mar Drugs) - "As a result, a derivatively named PM534 (2) is currently in its first human Phase I clinical trial. Herein, we present a comprehensive review of the isolation, structural elucidation, and antitumor activities of the parent compound PM742."

Journal • Review • Oncology

PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin. (PubMed, J Med Chem) - "Furthermore, PM534 induces significant inhibition of tumor growth in mouse xenograft models of human non-small cell lung cancer. Our results present PM534, a highly effective new compound in the preclinical evaluation that is currently in its first human Phase I clinical trial."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

PM534 Administered Intravenously to Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=30 | Recruiting | Sponsor: PharmaMar

Metastases • New P1 trial • Breast Cancer • Oncology • Prostate Cancer • Solid Tumor

The novel antitubulin agent PM534 exhibits potent antitumoral and antiangiogenic properties in vitro and in vivo (AACR 2023) - "Based on in vitro activity against different human tumor cell lines, in vivo activity in xenografted human tumors, as well as on its anti-angiogenic properties, the safety, pharmacology and preliminary antitumor activity of PM534 will be evaluated in a first-in-human clinical trial to be conducted in patients with advanced solid tumors."

Preclinical • Oncology • Solid Tumor

PM534 is a novel microtubule-destabilizing agent with high affinity and potent antineoplastic properties (AACR 2023) - "The mechanism of action of PM534 involves an optimized interaction with the colchicine site, which is reflected in its high affinity for the substrate, being this the ultimate reason for the observed cellular activity. Additionally, PM534 presents a potent antitumor activity in vitro that was translated into a clear positive in vivo PoC that resulted in strong antitumor effect."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor