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For more information on the Genta clinical development program please contact us at ClinicalTrials@genta.com or at http://www.clinicaltrials.gov

Oral Gallium

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Genta’s oral gallium compounds are investigational agents undergoing testing to evaluate safety and efficacy in the treatment of various conditions associated with bone loss. Studies are currently planned to examine the potential role of these compounds in a variety of clinical indications.

Gallium-containing compounds are potent inhibitors of bone resorption. These agents target bone tissue and are actively incorporated into bone mineral at sites where bone is metabolically active.

Gallium reduces bone loss by inhibiting calcium resorption from bone. Preclinical evidence suggests that the mechanism of gallium action is multifactorial and different from other current therapies used to treat bone loss, such as estrogen, selective estrogen receptor modulators (SERMs), denosumab, calcitonin, or bisphosphonates (e.g., Zometa® or Fosamax®). Gallium preferentially accumulates in metabolically active regions of bone, inhibits osteoclast-mediated bone resorption, and favorably alters bone mineral composition and properties.

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Oral Gallium Therapeutic Potential

An orally bioavailable gallium-containing compound may potentially be used to treat both acutely life-threatening diseases, such as cancer-related hypercalcemia, as well as for diseases with less extreme bone loss, including bone metastases, Paget’s disease and osteoporosis. Oral gallium could potentially be used for extended periods at low doses in order to maintain bone integrity and to prevent complications associated with accelerated loss of bone mass, such as fractures and pain.  Given the different mechanism of action, gallium compounds may also be associated with fewer bone complications that are associated with the long-term use of bisphosphonates, such as osteonecrosis.

The safety and efficacy of an oral gallium compound has not been established for any use.

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Mechanism of Action

Gallium reduces bone loss by inhibiting calcium resorption from bone. Preclinical evidence suggests that the mechanism of gallium action is multifactorial and different from other current therapies used to treat bone loss. 

 

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Preclinical Data

Drug disposition studies show that the active ingredient has a long plasma elimination half-life (101 hours in rat, 338 hours in dog).

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