Tìm theo
G4544
Thuốc Gốc
Small Molecule
G4544 is an oral gallium compound that enables oral absorption of the active ingredient contained in Ganite™ (gallium nitrate injection). It targets bone tissue and is actively incorporated into bone mineral at sites where bone is metabolically active.
Dược Lực Học : G4544 is one of a class of gallium containing compounds that were originally developed by the U.S. National Cancer Institute. In investigational studies, high doses of gallium nitrate demonstrated consistent antitumor activity in patients with non Hodgkin's lymphoma. However, experimental work by Genta personnel and others established that lower doses of gallium directly inhibited calcium release from bone, principally by decreasing bone resorption and possibly by also stimulating bone formation.
Cơ Chế Tác Dụng : G4544 is an oral gallium compound that enables oral absorption of the active ingredient contained in Ganite™ (gallium nitrate injection). It targets bone tissue and is actively incorporated into bone mineral at sites where bone is metabolically active. G4544 reduces bone loss by inhibiting calcium resorption from bone. Preclinical evidence suggests that the mechanism of G4544 action is multifactorial and different from other current therapies used to treat bone loss, such as estrogen or selective estrogen receptor modulators (SERMs), calcitonin, or bisphosphonates (e.g., Zometa or Fosamax). G4544 preferentially accumulates in metabolically active regions of bone, inhibits osteoclast-mediated bone resorption, and favorably alters bone mineral composition and properties.
Dược Động Học :
▧ Absorption :
Orally bioavailable.
Chỉ Định : For treatment of non-Hodgkin's lymphoma, bone metastases, Paget's disease, and osteoporosis
Liều Lượng & Cách Dùng : Tablet - Oral
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05244
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