Docetaxel

What it is and how it works

Mechanism of Action Docetaxel is an antineoplastic agent that acts by disrupting the microtubular network in cells that is essential for mitotic and interphase cellular functions. Docetaxel binds to free tubulin and promotes the assembly of tubulin into stable microtubules while simultaneously inhibiting their disassembly. This leads to the production of microtubule bundles without normal function and to the stabilization of microtubules, which results in the inhibition of mitosis in cells. Docetaxel's binding to microtubules does not alter the number of protofilaments in the bound microtubules, a feature which differs from most spindle poisons currently in clinical use.

Indications

1. INDICATIONS AND USAGE Docetaxel Injection is a microtubule inhibitor indicated for: • Breast Cancer (BC): single agent for locally advanced or metastatic BC after chemotherapy failure; and with doxorubicin and cyclophosphamide as adjuvant treatment of operable node-positive BC • Non-Small Cell Lung Cancer (NSCLC): single agent for locally advanced or metastatic NSCLC after platinum therapy failure; and with cisplatin for unresectable, locally advanced or metastatic untreated NSCLC • Castration-Resistant Prostate Cancer (CRPC): with prednisone in metastatic castration-resistant prostate cancer • Gastric Adenocarcinoma (GC): with cisplatin and fluorouracil for untreated, advanced GC, including the gastroesophageal junction • Squamous Cell Carcinoma of the Head and Neck (SCCHN): with cisplatin and fluorouracil for induction treatment of locally advanced SCCHN Breast Cancer Docetaxel Injection is indicated for the treatment of patients with locally advanced or metastatic breast cancer after failure of prior chemotherapy.

Dosage and administration (summary)

2. DOSAGE AND ADMINISTRATION For all indications, toxicities may warrant dosage adjustments . Administer in a facility equipped to manage possible complications (e.g., anaphylaxis). Administer in a facility equipped to manage possible complications (e.g., anaphylaxis). Administer intravenously (IV) over 1 hour every 3 weeks. PVC equipment is not recommended.

Contraindications

4. CONTRAINDICATIONS Docetaxel Injection is contraindicated in patients with: • neutrophil counts of <1500 cells/mm 3 . • a history of severe hypersensitivity reactions to docetaxel or to other drugs formulated with polysorbate 80. Severe reactions, including anaphylaxis, have occurred . • Hypersensitivity to docetaxel or polysorbate 80 • Neutrophil counts of < 1500 cells/mm 3

Warnings and precautions

5. WARNINGS AND PRECAUTIONS • Second primary malignancies: In patients treated with docetaxel-containing regimens, monitor for delayed AML, MDS, NHL, and renal cancer. • Cutaneous reactions: Reactions including erythema of the extremities with edema followed by desquamation may occur. Severe cutaneous adverse reactions have been reported. Severe skin toxicity may require dose adjustment or permanent treatment discontinuation. • Neurologic reactions: Reactions including paresthesia, dysesthesia, and pain may occur.

Pregnancy

Pregnancy Risk Summary Based on findings in animal reproduction studies and its mechanism of action, Docetaxel Injection can cause fetal harm when administered to a pregnant woman .

Storage and supply

16. HOW SUPPLIED/STORAGE AND HANDLING How Supplied Docetaxel Injection is supplied in a multiple-dose vial as a sterile, pyrogen-free solution. Docetaxel Injection requires NO prior dilution with a diluent and is ready to add to the infusion solution.

Source: Docetaxel (Docetaxel) — US FDA prescribing information, 2023-11-21, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.