Drug intelligence / Profile preview

holmium-166 DOTMP + melphalan

Development stage
Unknown
Lead developer
Poniard Pharmaceuticals
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

holmium-166 DOTMP + melphalan is a combination therapy consisting of a radiopharmaceutical and an alkylating chemotherapeutic agent, investigated primarily for the treatment of multiple myeloma. **Holmium-166 DOTMP** (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylenephosphonate) is a beta-emitting radiotherapeutic that selectively accumulates in bone matrix, delivering high-dose, targeted radiation to bone and bone marrow with relatively limited uptake in other tissues. **Melphalan** is a DNA-alkylating agent commonly used in high-dose regimens for multiple myeloma. Together, these agents enable intensified cytoreductive therapy prior to autologous hematopoietic stem cell transplantation, aiming to overcome dose limitations of chemotherapy by selectively escalating myeloablative radiation to marrow-involved sites. The combination has undergone phase 1/2 trials for conditioning in multiple myeloma and has shown promising rates of hematologic recovery and complete remissions, though with characteristic toxicities including renal and bladder effects at higher doses[1][2][3][4][6].

Brand names
Alkeran
Other names
holmium-166 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylenephosphonate + melphalan166ho-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylenephosphonic acid + melphalan
02

Targets

DNA

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