Aminopropylaminoethyl Thiophosphate

Aminopropylaminoethyl Thiophosphate Uses, Dosage, Side Effects, Food Interaction and all others data.

A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.

Aminopropylaminoethyl Thiophosphate is an organic thiophosphate cytoprotective agent indicated to reduce the cumulative renal toxicity associated with repeated administration of cisplatin in patients with advanced ovarian cancer or non-small cell lung cancer and also to reduce the incidence of moderate to severe xerostomia in patients undergoing post-operative radiation treatment for head and neck cancer. Aminopropylaminoethyl Thiophosphate is a prodrug that is dephosphorylated by alkaline phosphatase in tissues to a pharmacologically active free thiol metabolite, believed to be responsible for the reduction of the cumulative renal toxicity of cisplatin and for the reduction of the toxic effects of radiation on normal oral tissues. Healthy cells are preferentially protected because amifostine and metabolites are present in healthy cells at 100-fold greater concentrations than in tumour cells.

Trade Name Aminopropylaminoethyl Thiophosphate
Availability Prescription only
Generic Amifostine
Amifostine Other Names Amifostina, Amifostine, Amifostinum, Aminopropylaminoethyl thiophosphate
Related Drugs pilocarpine, glycerin topical, Salagen, trilaciclib, Biotene Mouthwash, XyliMelts, Cosela, Ethyol
Type
Formula C5H15N2O3PS
Weight Average: 214.223
Monoisotopic: 214.054099558
Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Aminopropylaminoethyl Thiophosphate
Aminopropylaminoethyl Thiophosphate

Uses

Aminopropylaminoethyl Thiophosphate is a cytoprotective adjuvant used for reduction in the cumulative renal toxicity in patients with ovarian cancer and moderate to severe xerostomia in patients undergoing post-operative radiation treatment for head and neck cancer.

For reduction in the cumulative renal toxicity in patients with ovarian cancer (using cisplatin) and moderate to severe xerostomia in patients undergoing post-operative radiation treatment for head and neck cancer.

Aminopropylaminoethyl Thiophosphate is also used to associated treatment for these conditions: Dry Mouth, Nephrotoxicity, Prophylaxis of Radiation proctitis

How Aminopropylaminoethyl Thiophosphate works

The thiol metabolite is responsible for most of the cytoprotective and radioprotective properties of amifostine. It is readily taken up by cells where it binds to and detoxifies reactive metabolites of platinum and alkylating agents as well as scavenges free radicals. Other possible effects include inhibition of apoptosis, alteration of gene expression and modification of enzyme activity.

Toxicity

Rat LD50: 826 mg/kg

Food Interaction

No interactions found.

Aminopropylaminoethyl Thiophosphate Disease Interaction

Major: dehydration, hypotensionModerate: hypocalcemia

Half Life

8 minutes

Elimination Route

After a 10-second bolus dose of 150 mg/m2 of ETHYOL, renal excretion of the parent drug and its two metabolites was low during the hour following drug administration, averaging 0.69%, 2.64% and 2.22% of the administered dose for the parent, thiol and disulfide, respectively.

Innovators Monograph

You find simplified version here Aminopropylaminoethyl Thiophosphate

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