Bisphonal
Bisphonal Uses, Dosage, Side Effects, Food Interaction and all others data.
Incadronate, or YM-175, is a nitrogen containing bisphosphonate. Along with being investigated to treat hypercalcemia of malignancy, it has also been investigated in the treatment of myeloma, leukemia, and other cancers.
Bisphonal was first described in the literature in 1991.
Trade Name | Bisphonal |
Generic | Incadronic acid |
Incadronic acid Other Names | Cimadronate, Incadronate, Incadronic acid |
Type | |
Formula | C8H19NO6P2 |
Weight | Average: 287.189 Monoisotopic: 287.068761332 |
Groups | Experimental |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Incadronate has been investigated in the treatment of myeloma, leukemia, and other cancers. It has also been investigated in patients with hypercalcemia of malignancy.
How Bisphonal works
Bisphosphonates are taken into the bone where they bind to hydroxyapatite. Bone resorption by osteoclasts causes local acidification, releasing the bisphosphonate, which is taken into the osteoclast by fluid-phase endocytosis. Endocytic vesicles become acidified, releasing bisphosphonates into the cytosol of osteoclasts where they act.
Osteoclasts mediate resorption of bone. When osteoclasts bind to bone they form podosomes, ring structures of F-actin. Disruption of the podosomes causes osteoclasts to detach from bones, preventing bone resorption.
Nitrogen containing bisphosphonates such as incandronate are known to induce apoptosis of hematopoietic tumor cells by inhibiting the components of the mevalonate pathway farnesyl diphosphate synthase, farnesyl diphosphate, and geranylgeranyl diphosphate. These components are essential for post-translational prenylation of GTP-binding proteins like Rap1. The lack of prenylation of these proteins interferes with their function, and in the case of Rap1, leads to apoptosis. incadronate also activated caspases 3, 4, and 7; further contributing to apoptosis.
Food Interaction
No interactions found.Half Life
Incadronate has a biexponential half life. The T1/2α is 0.26-0.40h and the T1/2β is 1.58-1.98h.
Elimination Route
Incadronate is 55.1-69.5% eliminated in the urine as the unchanged parent drug.
Innovators Monograph
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