Irinotecan Hydrochloride Injection

Irinotecan is a semisynthetic derivative of camptothecin. Camptothecin can specifically bind to topoisomerase 1, which induces reversible single-strand breaks, thereby unwinding the DNA double-strand structure; irinotecan and its active metabolite SA-38 can bind to the topoisomerase I-DNA complex, thereby preventing the reconnection of the broken single strands. Existing studies suggest that the cytotoxic effect of irinotecan is attributed to the interaction between the replicase and the topoisomerase 1-DNA-irinotecan (or SN-38) triple complex during DNA synthesis, thereby causing DNA double-strand breaks. Mammalian cells cannot effectively repair such DNA double-strand breaks.

The main ingredient of this product is irinotecan hydrochloride, and its chemical name is ()-(4S)-4,11-diethyl-4-hydroxy-9-[(4-piperidinylpiperidine)carbonyl]-1H-pyrano[3,4:6,7]indolizine[1,2b]quinoline-3,14-(4H,12H)-dione hydrochloride trihydrate.

This product is suitable for the treatment of patients with advanced colorectal cancer: combined with 5-fluorouracil and folinic acid to treat patients with advanced colorectal cancer who have not received chemotherapy before; as a single drug, to treat patients who have failed chemotherapy containing 5-fluorouracil.

The recommended dose of this product is 350 mg/m2, diluted with 5% glucose or 0.9% sodium chloride injection, and then intravenously dripped for 30 to 90 minutes, once every three weeks.

1. Gastrointestinal tract: Delayed diarrhea: Diarrhea (occurring 24 hours after medication) is the dose-limiting toxic reaction of this product. Among all patients who followed the advice on diarrhea treatment measures, 20% had severe diarrhea. The median time of the first loose stool was 5 days after instillation of this product. Pseudomembranous colitis occurred in individual cases, one of which was confirmed by bacteriology (Clostridium difficile). Nausea and vomiting: Severe nausea and vomiting still occurred in 10% of patients after the use of antiemetics. Other gastrointestinal reactions: Diarrhea and/or vomiting accompanied by dehydration symptoms have been reported. Less than 10% of patients have constipation related to treatment with this product. Intestinal obstruction has rarely been reported. Other mild reactions include anorexia, abdominal pain and mucositis. 2. Hematology: Neutropenia is a dose-limiting toxicity. 78.7% of patients experienced neutropenia, and severe cases (neutrophil count; 500/mm3) accounted for 22.6%. During the evaluable cycle, 18% had a neutrophil count of 1000/mm3, of which 7.6% had a neutrophil count of 500/mm3. Neutropenia was reversible and non-accumulative, with a median time to the lowest point of 8 days, and usually fully recovered to normal on the 22nd day. Severe neutropenia with fever occurred in 6.2% of patients (1.7% per cycle). Infection occurred in 10.3% of patients (2.5% per cycle); 5.3% of patients (1.1% per cycle) had infections caused by severe neutropenia, and 2 patients died. The incidence of anemia was 58.7% ((including 8% Hb; 8g/dl, 0.9% Hb; 6.5g/dl). Thrombocytopenia (; 100000/mm3) occurred in 7.4% of patients (1.8% by cycle), (including 0.9% platelets; 50000/mm3, 0.2% by cycle). Almost all patients recovered on the 22nd day. During post-marketing use, a case of peripheral thrombocytopenia caused by antiplatelet antibodies has been reported. 3. Acute cholinergic syndrome: 9% of patients developed transient and severe acute cholinergic syndrome. The main symptoms are: early-onset diarrhea and other symptoms, such as abdominal pain, conjunctivitis, rhinitis, hypotension, vasodilation, sweating, chills, general discomfort, dizziness, visual impairment, Pupil constriction, tearing, and increased salivation, all of which disappear after atropine treatment. 4. Other effects: Early reactions such as dyspnea, muscle contraction, cramps, and paresthesia have been reported. Less than 10% of patients experience severe fatigue, and the exact relationship between this and the use of this product has not yet been clarified. Hair loss is common and is reversible. 12% of patients experience fever without infection or severe neutropenia. Mild skin reactions, allergic reactions, and injection site reactions, although uncommon, have also been reported. 5. Laboratory tests: The incidence of transient, mild to moderate increases in serum aminotransferase, alkaline phosphatase, and bilirubin levels was 9.2%, 8.1%, and 1.8%, respectively (in patients without progressive liver metastases). 7.3% of patients experienced transient, mild to moderate increases in serum creatinine levels.

1. Contraindicated in patients with chronic enteritis and/or intestinal obstruction. 2. Contraindicated in patients with a history of severe allergic reaction to irinotecan hydrochloride trihydrate or its excipients. 3. Contraindicated in pregnant and lactating women. 4. Contraindicated in patients with bilirubin exceeding 1.5 times the upper limit of normal. 5. Contraindicated in patients with severe bone marrow failure. 6. Contraindicated in patients with WHO performance status score 2

Precautions during pregnancy and lactation: Contraindicated for use in pregnant and lactating women.

Not yet clear.

Keep away from light and store in a sealed container at room temperature (10-30°C).

5ml:0.1g (calculated as C33H38N4O6·HCl·3H2O)

Qilu Pharmaceutical (Hainan) Co., Ltd.

• Founded in:

  2005-10-18

• Address:

  No. 273-A, Nanhai Avenue, National High-tech Zone, Haikou City

• Tax NO.:

  91460000780701210W

• Registered Funds:

  40 million yuan

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