Artigo Acesso aberto Revisado por pares

A phase 1 study of lucatumumab, a fully human anti‐ CD 40 antagonist monoclonal antibody administered intravenously to patients with relapsed or refractory multiple myeloma

2012; Wiley; Volume: 159; Issue: 1 Linguagem: Inglês

10.1111/j.1365-2141.2012.09251.x

ISSN

1365-2141

Autores

William Bensinger, Richard T. Maziarz, Sundar Jagannath, Andrew Spencer, Simon Durrant, Pamela S. Becker, Brett Ewald, Sanela Bilic, John Rediske, Johan Baeck, Edward A. Stadtmauer,

Tópico(s)

Peptidase Inhibition and Analysis

Resumo

Summary In this open‐label, multicentre, phase 1 study a fully human anti‐ CD 40 antagonist monoclonal antibody, lucatumumab, was evaluated in patients with relapsed/refractory multiple myeloma ( MM ). The primary objective was to determine the maximum tolerated dose ( MTD ) based on dose‐limiting toxicities ( DLT s). Secondary objectives included safety, pharmacokinetics, pharmacodynamics and antimyeloma activity. Twenty‐eight patients, enrolled using a standard ‘3 + 3’ dose escalation, received one or two ( n = 3) cycles of lucatumumab 1·0, 3·0, 4·5 or 6·0 mg/kg once weekly for 4 weeks. Common lucatumumab‐related adverse events were reversible, mild‐to‐moderate infusion reactions. Severe adverse events were anaemia, chills, hypercalcaemia and pyrexia (7% each). DLT s included grade 4 thrombocytopenia, grade 3 increased alanine aminotransferase and grade 4 increased lipase ( n = 1 each). The MTD was 4·5 mg/kg. At doses ≥3·0 mg/kg, sustained receptor occupancy (≥87%), observed throughout weekly infusions up to 5 weeks after the last infusion, correlated with an estimated half‐life of 4–19 d. Twelve patients (43%) had stable disease, and one patient (4%) maintained a partial response for ≥8 months. These findings indicate that single‐agent lucatumumab was well tolerated up to 4·5 mg/kg with modest clinical activity in relapsed/refractory MM , warranting further study as a combination therapy.

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