What is Lenalidomide use for? How toxic is Lenalidomide?

Lenalidomide is an immunomodulatory drug with potent antineoplastic, anti-angiogenic, and anti-inflammatory properties. It is a 4-amino-glutamyl analogue of thalidomide 3.However, lenalidomide is much safer and potent than thalidomide, with fewer adverse effects and toxicities.

Brand Names

Lenalidomide Accord, Lenalidomide Krka, Lenalidomide Mylan, Revlimid

Uses

Lenalidomide is a treatment for:

myeloma

myelodysplastic syndromes

follicular lymphoma

mantle cell lymphoma

Mechanism of action

Lenalidomide works by:

stopping cancer cells developing

stopping blood vessels growing in the cancer

stimulating part of the immune system to attack the cancer cells

Side effects

Common side effects of lenalidomide include diarrhea, itchiness, joint pain, fever, headache, and trouble sleeping. Severe side effects include low blood platelets, low white blood cells, and blood clots. The dose may need to be adjusted in people with kidney problems. Lenalidomide is closely related to thalidomide, which is known to cause severe birth defects, so its use during pregnancy is very likely to harm the fetus.

Toxicity

The lowest lethal dose (LDLo) in rats is >2000 mg/kg following oral administration and >40 mg/kg following intravenous administration.10 The oral Lowest published toxic dose (TDLo) in humans is 9 mg/kg/4W (intermittent).

There is limited clinical experience in managing lenalidomide overdose. In single-dose studies, healthy subjects have been exposed to doses up to 400 mg. In clinical trials, the dose-limiting toxicity was neutropenia and thrombocytopenia. Toxicities associated with lenalidomide, some leading to fatality, include embryo-fetal toxicity, neutropenia, thrombocytopenia, venous (deep vein thrombosis and pulmonary embolism) and arterial thromboembolic events (myocardial infarction and stroke), serious adverse cardiovascular reactions, second primary malignancies, hepatotoxicity, severe cutaneous reactions, tumour lysis syndrome, tumour flare reaction, hypothyroidism, and hyperthyroidism.

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