AMIFOSTINE

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Description

AMIFOSTINE is being supplied by MedicaPharma in pharma GMP grade.
We have several principals on hand for this material. Just send us your quote request and we will serve you. Amifostine (ethiofos) is a cytoprotective adjuvant used in cancer chemotherapy and radiotherapy involving DNA-binding chemotherapeutic agents.

Indications

Amifostine is used therapeutically to reduce the incidence of neutropenia-related fever and infection induced by DNA-binding chemotherapeutic agents including alkylating agents (e.g. cyclophosphamide) and platinum-containing agents (e.g. cisplatin). It is also used to decrease the cumulative nephrotoxicity associated with platinum-containing agents. It is also indicated to reduce the incidence of xerostomia in patients undergoing radiotherapy for head and neck cancer. Amifostine was originally indicated to reduce the cumulative renal toxicity from cisplatin in non-small cell lung cancer. However, while nephroprotection was observed, the probability that amifostine could protect tumors could not be excluded. Additional data have shown that similar-mediated tumor protection, in any clinical scenario, is unlikely.

Mechanism of action

Inside cells, the material detoxifies reactive metabolites of platinum and alkylating agents, as well as scavenges free radicals. Other possible effects include accelerated DNA repair, induction of cellular hypoxia, inhibition of apoptosis, alteration of gene expression and modification of enzyme activity. It is believed to radioprotect normal tissue via Warburg-type effects.

Pharmacokinetics

WR-1065, 2-((aminopropyl)amino)ethanethiol, the active metabolite of the concerning material.

Amifostine is an organic thiophosphate prodrug which is hydrolysed in vivo by alkaline phosphatase to the active cytoprotective thiol metabolite, WR-1065. The selective protection of non-malignant tissues is believed to be due to higher alkaline phosphatase activity, higher pH, and vascular permeation of normal tissues. It can be administered intravenously or subcutaneously after reconstitution with normal saline. Infusions lasting less than 15 minutes decrease the risk of adverse effects. The patient should be well-hydrated prior to administration.

Adverse effects

Common side effects of the material include hypocalcemia, diarrhea, nausea, vomiting, sneezing, somnolence, and hiccoughs. Serious side effects include: hypotension (found in 62% of patients), erythema multiforme, Stevens–Johnson syndrome and toxic epidermal necrolysis, immune hypersensitivity syndrome, erythroderma, anaphylaxis, and loss of consciousness (rare).

Contraindications

Contraindications to receiving this material include hypersensitivity to amifostine and aminothiol compounds like WR-1065. Ethyol contains mannitol. (Source: Wikipedia)