Evaluation of bendamustine in combination with fludarabine in primary chronic lymphocytic leukemia cells.

The fludarabine and cyclophosphamide couplet has become the backbone of the chronic lymphocytic leukemia (CLL) standard of care. Although this is an effective treatment, it results in untoward toxicity. Bendamustine is a newly approved and better-tolerated alkylating agent.

188Re-labelled gemcitabine/bisphosphonate (Gem/BP): a multi-functional, bone-specific agent as a potential treatment for bone metastases.

Purpose: This study investigated the bone-binding affinity and biodistribution of a (188)Re-labelled gemcitabine/bisphosphonate (Gem/BP) conjugate, a multi-functional drug designed to deliver tumour-specific combined radiotherapy and chemotherapy to the bone using the high bone-binding affinity of the bisphosphonate group.

Methods: The Gem/BP conjugate was labelled at high radiochemical purity with (188)Re. The bone-binding affinity of the (188)Re-Gem/BP was studied in vitro in purified hydroxyapatite emulsion and powdered bovine bone.

A 99mTc-labeled gemcitabine bisphosphonate drug conjugate as a probe to assess the potential for targeted chemotherapy of metastatic bone cancer.

Introduction: A novel compound with the potential for "targeted" therapy for cancer patients was prepared using a conjugate between the potent anticancer drug Gemzar (gemcitabine) and a bisphosphonate. This conjugate would be expected to accumulate at sites of bone metastatic cancer by virtue of an affinity of the bisphosphonate for bone undergoing osteoclastic and osteoblastic remodeling. Release of the anticancer drug at the site of the tumor would provide high local concentrations of the drug but avoid systemic toxicity.