Trabectedin (Yondelis) is an injectable alkylating agent approved by the U.S. Food and Drug Administration (FDA) in 2015 for clinical treatment, specifically targeting certain types of soft tissue sarcomas. With an innovative chemical structure, this drug exerts its therapeutic effects through a precise administration regimen.
Indications for Trabectedin (Yondelis)
Treatment of Specific Soft Tissue Sarcomas
Trabectedin is specifically indicated for the treatment of patients with unresectable or metastatic liposarcoma or leiomyosarcoma who have previously received anthracycline-containing treatment regimens.
Characteristics of Target Patients
Patients have unresectable liposarcoma or leiomyosarcoma.
The disease has progressed to the metastatic stage.
Patients have previously received anthracycline-containing treatment regimens.
The disease includes dedifferentiated, myxoid round cell, or pleomorphic liposarcoma.
Pharmacological Actions
As an alkylating agent, trabectedin binds to guanine residues in the minor groove of DNA to form adducts, causing the DNA helix to bend toward the major groove.
The formation of these adducts triggers a series of events that affect the subsequent activity of DNA-binding proteins (including certain transcription factors and DNA repair pathways), ultimately leading to cell cycle disruption and cell death.
Specifications and Properties of Trabectedin (Yondelis)
Dosage Specifications
Trabectedin is supplied as 1 mg of sterile lyophilized powder in a single-dose vial.
Physical Characteristics
Appearance: White to off-white powder/cake.
Packaging: Each carton contains one vial.
Active Ingredient
Trabectedin: Chemical name – (1'R,6R,6aR,7R,13S,14S,16R)-5-(acetyloxy)-3',4',6,6a,7,13,14,16-octahydro-6',8,14-trihydroxy-7',9-dimethoxy-4,10,23-trimethylspiro[6,16-(epithiopropanoxymethano)-7,13-imino-12H-1,3-dioxolo[7,8]isoquino[3,2-b][3]benzazepine-20,1'(2'H)-isoquinolin]-19-one.
Excipient Composition
27.2 mg of potassium dihydrogen phosphate.
400 mg of sucrose.
Phosphoric acid and potassium hydroxide (used to adjust the pH to 3.6–4.2).
Characteristics of Reconstituted Solution
The reconstituted solution is clear, colorless to pale tan.
Contains trabectedin at a concentration of 0.05 mg/mL.
Must be used within 30 hours after reconstitution.
Chemical Properties
Molecular Formula: C₃₉H₄₃N₃O₁₁S.
Molecular Weight: 761.84 Daltons.
Hydrophobicity: Highly hydrophobic with low solubility in water.
Storage Methods for Trabectedin (Yondelis)
Temperature Control
Trabectedin vials should be stored under refrigeration at 2°C to 8°C (36°F to 46°F).
Reconstitution Requirements
Use 20 mL of water for injection for reconstitution.
Shake the vial until the powder is completely dissolved.
Check for particulate matter and discoloration.
Dilution Requirements
Further dilute with 0.9% Sodium Chloride Injection or 5% Dextrose Injection to a total volume of 500 mL.
Must not be mixed with other drugs.
Special Storage Requirements
The drug should be stored in its original packaging.
Any unused portion of the reconstituted solution and infusion solution should be discarded.
Protect the drug from contamination and direct light exposure.
Transportation Requirements
Maintain the integrity of the cold chain during transportation.
Ensure the temperature remains within the specified range at all times.
Follow the guidelines for preparation and administration.
