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Description – Amifostine
Amifostine is a broad-spectrum radio- and chemoprotector. It restores transcriptional activity of specific p53 mutants, prevents chemotherapy-induced apoptosis and upregulates HIF-1α. Amifostine offers a selective protection to normal cells over tumor cells due to normal cells having a 275-fold greater concentration of alkaline phosphatase, by reducing renal toxicity, higher pH and better vascularity of the normal tissue. In physiological conditions, Amifostine is rapidly dephosporylated by alkaline phosphatase into an active free thiol. As a free thiol, Amifostine can act as a scavenger of free radicals against cytotoxic drugs. The compound has also displayed cytoprotectivity against alkylating drugs and cisplatin (sc-200896). Amifostine is an activator of p53.
Brand names
Ethyol, Ethiofos
Storage of Amifostine
Store at room temperature
Identity of Amifostine
| Type of medicine | Cytoprotectants |
| Synonyms | Amifostina, Amifostine, Amifostinum, Aminopropylaminoethyl thiophosphate, Ethiofos |
| Molecular Formula | C5H15N2O3PS |
| Molecular Weight | 214.223 g/mol |
| IUPAC Names | ({2-[(3-aminopropyl)amino]ethyl}sulfanyl)phosphonic acid |
| Structural formula of main components |  |
| Pure active ingredient | Amifostine |
| Appearance | Crystalline powder |
| Melting point | 86.28° C |
| Available as | Powder for Solution |
| Prescription | Prescription is required before the consumption |
Amifostine is used to prevent
- Renal (kidney)toxicity. It is used to reduce the nephrotoxic effects caused by repeated treatment with cisplatin for advancedovarian cancer.
- Xerostomia (dry mouth). It is used to decrease dryness in the mouth caused by radiation therapy after surgery in some patients with head and neck cancer.
Amifostine is also being studied in the treatment of other types of cancer.
Possible Side Effects
There are a number of things you can do to manage the side effects of amifostine. Talk to your care team about these recommendations. They can help you decide what will work best for you. These are some of the most common or important side effects:
Hypotension
This medication can cause a drop in your blood pressure (hypotension). Your blood pressure will be monitored by your healthcare team before, during (if the infusion lasts for more than 5 minutes), and after treatment with this medication.
Cutaneous Reactions
This medication may cause cutaneous (skin) reactions including erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, toxoderma, and exfoliative dermatitis. Report any skin changes to your healthcare team immediately, particularly any rash involving the lips or mouth and/or lesions on the palms of hands, soles of the feet, or the front/back of the abdomen.
Allergic Reactions
Not often, but in some cases, patients can have an allergic reaction to this medication. Signs of a reaction can include shortness of breath or difficulty breathing, chest pain, rash, flushing or itching, or a decrease in blood pressure. If you notice any changes in how you feel during or after the infusion, let your nurse know immediately.
Nausea and/or Vomiting
Talk to your oncology care team so they can prescribe medications to help you manage nausea and vomiting. In addition, dietary changes may help. Avoid things that may worsen the symptoms, such as heavy or greasy/fatty, spicy or acidic foods (lemons, tomatoes, oranges). Try saltines, or ginger ale to lessen symptoms.
Call your oncology care team if you are unable to keep fluids down for more than 12 hours or if you feel lightheaded or dizzy at any time.
Hypocalcemia (Low Blood Calcium)
Amifostine can cause a low level of calcium in your blood. Symptoms of low blood calcium include muscle spasms and/or twitching, numbness or tingling of fingers, toes, or around the mouth. If this occurs, your healthcare team may ask you to take calcium supplements (like Tums) to correct this problem. Do not take supplements without first consulting your care team.
Reproductive Concerns
Amifostine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Exposure of an unborn child to this medication could cause birth defects. It is also recommended that breastfeeding be discontinued during treatment with this medication.
Mechanism of Action
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.
What other drugs will affect amifostine?
Taking any drugs that can lower your blood pressure may cause dangerous side effects while you are receiving amifostine.
Tell your doctor about all your current medicines and any you start or stop using, especially:
- An antidepressant;
- Heart or blood pressure medication;
- Medicine for erectile dysfunction;
- Medicine to treat Parkinson’s disease; or
- Opioid (narcotic) medication.
This list is not complete. Other drugs may interact with amifostine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.
Dosage and Administration of Amifostine
Intravenous
Prophylaxis of xerostomia in patients undergoing radiotherapy for head and neck cancer
Adult: 200 mg/m2 once daily via infusion over 3 min, starting w/in 15-30 min prior to radiotherapy.
Cytoprotective agent in chemotherapy
Adult: Initially, 910 mg/m2 once daily via infusion over 15 min, starting 30 min prior to chemotherapy. Subsequent doses reduced to 740 mg/m2 if patient is unable to tolerate the full dose. For cisplatin doses <100 mg/m2: 740 mg/m2.
Reconstitution
Add 9.7 mL of sterile NaCl 0.9% inj to a 500 mg vial to prepare a 10 mL soln containing 50 mg/mL. For use prior to chemotherapy, dilute further in sterile NaCl 0.9% to a final concentration of 5-40 mg/mL.
If overdose is suspected
Symptoms may include seizures; severe or persistent dizziness; shortness of breath.
Precautions
- Before starting amifostine treatment, make sure you tell your doctor about any other medications you are taking (including over-the-counter drugs, vitamins, or herbal remedies).
- Amifostine may be inadvisable if you have had a hypersensitivity (allergic) reaction to aminothiol compounds or mannitol.
- Your blood pressure medication will likely be stopped for 24 hours before treatment with amifostine. You should discuss this with your doctor.
- Inform your health care professional if you are pregnant or may be pregnant prior to starting this treatment. Pregnancy category C (use in pregnancy only if benefit to mother outweighs risk to fetus).
- For both men and women: Do not conceive a child (get pregnant) while taking amifostine. Barrier methods of contraception, such as condoms, are recommended. Discuss with your doctor when you may safely become pregnant or conceive a child after therapy.
- Do not breast feed while taking this medication.
Amifostine and Pregnancy
No adequate and well-controlled human studies have been conducted to determine if use of amifostine is safe and effective during pregnancy; it is unknown if the drug causes fetal harm or affects reproductive capacity. In rabbits, amifostine was embryotoxic at 60% of the recommended human dose based on body surface area. Use during pregnancy is recommended only if the benefit to the mother justifies the potential risk to the fetus.
Breast-feeding
Data are limited regarding use of amifostine during breast-feeding, and its excretion into breast milk is unknown. The manufacturer recommends discontinuing breast feeding if treatment with the drug is required. However, because it is administered when breast-feeding is unlikely (immediately prior to chemotherapy or radiation) and because of its short half-life, the risk to a nursing infant is low. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, health care providers are encouraged to report the adverse effect to the FDA.