Oxaliplatin – Targeted Therapy

Oxaliplatin is an antineoplastic agent representing the third generation of platinum-based organic compounds. The drug belongs to the class of alkylating agents and is widely used in modern oncology due to its high cytotoxic activity and a more favorable safety profile compared to cisplatin.

The mechanism of action of oxaliplatin is based on its ability to interact with the DNA of tumor cells. Active derivatives of the drug form intrastrand and interstrand cross-links in the DNA molecule, which block replication and transcription processes. This leads to DNA strand breaks and subsequent malignant cell death via apoptosis. Oxaliplatin is effective even against tumor lines that have developed resistance to other platinum agents.

The drug is administered exclusively intravenously via infusion. Oxaliplatin exhibits significant synergism with fluoropyrimidines, making it a key component of standard chemotherapy protocols for colorectal cancer.

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Indications

Oxaliplatin is indicated for the systemic treatment of malignant neoplasms of the gastrointestinal tract:

Colorectal Cancer: adjuvant therapy of colon cancer following surgical resection of the primary tumor (Stage III).
Metastatic Cancer: treatment of advanced colorectal cancer (usually in combination with 5-fluorouracil and leucovorin — FOLFOX regimens).
Gastric Cancer: therapy for advanced forms of gastric adenocarcinoma and gastroesophageal junction cancer.
Pancreatic Cancer: used as part of combination regimens (e.g., FOLFIRINOX) for metastatic disease.

Dosage and administration

The oxaliplatin dosing regimen is established individually based on body surface area and the specific treatment schedule.

Standard Dose: 85 mg/m² (in FOLFOX regimens every 2 weeks) or 130 mg/m² (in XELOX regimens every 3 weeks).
Route of Administration: intravenous infusion lasting from 2 to 6 hours. The drug must not be administered simultaneously with alkaline solutions or medications containing chlorides.
Diluent: only 5% glucose (dextrose) solution is used to prepare the infusion solution.
Dose Adjustment: if neurotoxicity or significant hematologic toxicity develops, the dose is reduced or the intervals between administrations are increased.
Precautions: during and immediately after administration, the patient should avoid contact with cold objects and consumption of cold food/drinks.

The use of oxaliplatin is contraindicated in the presence of the following factors:

Myelosuppression: baseline neutrophil count < 1500/µL and/or platelet count < 75000/µL.
Peripheral Neuropathy: presence of sensory neuropathy with functional impairment prior to the start of the first course.
Renal Impairment: severe renal failure (creatinine clearance < 30 mL/min).
Pregnancy and Lactation: the drug has genotoxic effects; breastfeeding is strictly prohibited.
Hypersensitivity: known allergy to oxaliplatin or other platinum derivatives.

The toxicity profile of oxaliplatin includes specific reactions that require medical supervision:

Neurotoxicity: peripheral sensory neuropathy manifesting as paresthesias (tingling) and numbness, often triggered by cold exposure.
Digestive System: nausea, vomiting, diarrhea (often severe), and stomatitis.
Hematology: anemia, leukopenia, and thrombocytopenia (risk of bleeding and infections).
Allergic Reactions: risk of bronchospasm and anaphylactic shock during infusion.
Hepatic System: potential development of hepatic veno-occlusive disease with prolonged use.

Frequently Asked Questions

Oxaliplatin is a third-generation platinum-based antineoplastic agent. It belongs to the class of alkylating agents. The substance forms cross-links within the DNA of cancer cells, preventing the replication of genetic material. This renders cell division impossible and triggers programmed cell death.

The primary indication for oxaliplatin is the treatment of metastatic colorectal cancer. It is frequently used in combination with fluorouracil and folinic acid (the FOLFOX regimen). The substance is also effective as adjuvant therapy following the surgical removal of the primary tumor to prevent recurrence.

Oxaliplatin causes a specific peripheral neuropathy that is acutely exacerbated by exposure to cold. Patients may experience tingling, numbness, or spasms in the limbs and throat when breathing cold air or touching cold objects. While these symptoms are usually transient, they require specific precautions.

It is recommended to avoid cold foods and beverages (including ice cream and ice) during and for several days after the infusion. When going outdoors in cool weather, patients should cover their face with a scarf and wear gloves and warm socks. It is also important to avoid contact with cold surfaces, such as opening a refrigerator without gloves.

Oxaliplatin is administered only by intravenous infusion. It must never be diluted or mixed with chloride-containing solutions (such as normal saline), as chlorides cause the active substance to decompose. It should be diluted exclusively with a 5% glucose (dextrose) solution.