Quick Facts About: Irinotecan

Campto, Camptosar, Irinox, DBL Irinotecan, Irinotesin

Yes, in 1996.

Metastatic colorectal cancer.

Irinotecan may be administered as either monotherapy or in combination with other therapeutic agents.

Dosage is dependent on drug combination in the treatment regimen and is based on the patient’s body surface area (milligram per square meter, mg/m²).

As monotherapy

• Irinotecan is administered to patients whose fluorouracil-containing regimen is unsuccessful.

The dosage for irinotecan as therapy may follow one of the two options below:

1. 350 mg/m² via infusion over 30-90 minutes every 3 weeks
2. 125 mg/m² via infusion over 90 minutes on days 1, 8, 15 and 22 followed by 2-week rest

As combination therapy

• Irinotecan is administered together with fluorouracil and folinic acid (leucovorin) in patients who have not received prior chemotherapy.

In this instance, the dosage is 180 mg/m² once every 2 weeks over 30-90 minutes, and continues until disease progression or unacceptable toxicity occurs.

Irinotecan may also be used in the following combinations:

Usage should be avoided for the following contraindications:

• Chronic inflammatory bowel disease and/or bowel obstruction
• Severe bone marrow failure
• WHO performance status > 2
• Pregnancy and lactation
• Concomitant use with live attenuated vaccines and St. John’s worts

In addition, irinotecan should be avoided for patients with renal impairment, while patients with hepatic impairments may require a different irinotecan dosage depending on their bilirubin levels.

Special precautions are required for patients:

• With poorly regulated bilirubin glucuronidation (or metabolism) or hyperbilirubinemia
• Have previously received radiation therapy to to the pelvic or abdominal area
• Have history of
  • Whipple procedure
  • Asthma
  • Underlying cardiac disease or cardiac disease risk factors such as hypertension or smoking
• Who are underweight (BMI < 18.5 kg/m²)

Common side effects of irinotecan may include:

• Fever, pain, mouth sores, or other signs of infection
• Decreased blood cell levels and abnormal liver function
• Diarrhea or constipation
• Nausea, vomiting and stomach pain
• Loss of appetite, weight loss
• Fatigue
• Hair loss

Patients may also experience more severe side effects, including:

• Severe and/or continuous vomiting or diarrhea
• Black, bloody or tarry stools
• Continuous nausea or vomiting
• Sores around your mouth
• Cough or shortness of breath
• Dehydration symptoms
• Low blood cell counts

Patients who experience severe systems should seek immediate medical attention.

Irinotecan is a chemotherapy drug.

Irinotecan inhibits a specific phase in DNA synthesis known as the S phase, during which the cell synthesizes a complete copy in the nucleus.

Irinotecan binds to an enzyme called topoisomerase I that is responsible for relaxing and uncoiling the DNA helix by cutting one DNA strand. Irinotecan prevents the re-ligation of the cleaved DNA strand, leading to the accumulation of irreparable double-strand DNA breaks, thereby resulting in cell death and termination of cellular replication.