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Trabectedin indications, mechanism of action and side effects

Nov 8，2024

Trabectedin is an antineoplastic drug approved by the EMA for the treatment of soft tissue sarcoma (STS). Trabectedin is indicated for the treatment of patients with advanced STS after failure of anthracycline and ifosfamide therapy, or for patients who are not suitable for these drugs.

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Mechanism of Action

Trabectedin, also known as ecteinascidin-743 or ET-743, is a marine-derived compound isolated from the Caribbean tunicate Ecteinascidia turbinata with a unique mechanism of action. It acts as an alkylating agent by binding to the minor groove of DNA, inducing single-strand breaks (SSBs) and double-strand breaks (DSBs), which in turn trigger a cascade of events that interfere with multiple transcription factors, DNA-binding proteins and DNA repair pathways, leading to G2-M cell cycle arrest and ultimately apoptosis.

Side Effects

Trabectedin is a well-tolerated and less toxic drug. Most of its side effects are mild and easy to manage. Specific adverse events such as hepatotoxicity and rhabdomyolysis are usually not clinically significant.

Common side effects include:

Nausea

Fatigue

Vomiting

Constipation

Loss of appetite

Diarrhea

Swelling of the hands, ankles, or feet

Shortness of breath

Headache

Decreased red blood cell count and platelet count

Changes in blood tests for liver and kidney function

Serious side effects include:

Serious infections

Rhabdomyolysis (muscle pain or weakness)

Liver problems (such as liver failure)

Heart muscle problems (chest pain, shortness of breath, palpitations, or heart failure)

Capillary leak syndrome (severe cases can be fatal)

Severe allergic reactions (trouble breathing, chest tightness, wheezing, swollen lips, or rash)

If you experience any of these serious adverse reactions, please see your doctor immediately.

References:

[1] JUAN MARTIN-LIBERAL; Ian J. Safety evaluation of trabectedin in treatment of soft-tissue sarcomas.[J]. Expert Opinion on Drug Safety, 2013. DOI:10.1517/14740338.2013.829037.

[2] TOMOKI NAKAMURA; A. S. The Role of Trabectedin in Soft Tissue Sarcoma[J]. Frontiers in Pharmacology, 2022. DOI:10.3389/fphar.2022.777872.

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