Irinotecan Powder CAS 97682-44-5

Irinotecan powder is a light yellow powder with molecular formula: C33H38N4O6, molecular weight: 586.68, melting point: 222~223℃, boiling point: 873.4±65.0 °C(Predicted), density: 1.40 0.1g/cm3 (predicted). It is a topoisomerase I inhibitor, which is mainly used to treat colorectal cancer and small cell cancer. It can also be used to treat pancreatic cancer with 5- fluorouracil and folinic acid after the initial course of treatment fail.

Irinotecan is a semi-synthetic water-soluble camptothecin derivative. Its metabolite SN38 is a DNA topoisomerase I inhibitor, and its complex with topoisomerase I and DNA can cause DNA single-strand break, prevent DNA replication, and inhibit RNA synthesis, which is specified in the S phase of the cell cycle.

What is Irinotecan?

Irinotecan powder, a specific inhibitor of topoisomerase I, produces active metabolites through the action of tissue enzymes, which act on the S phase of the cell cycle, producing specific reactions and inhibiting the DNA synthesis of tumor cells.

It is known that irinotecan has broad-spectrum and powerful anti-tumor activity in vivo and in vitro studies, and the drug itself and its metabolites are still effective for multi-drug resistant tumors, which can effectively treat small cell and non-small cell lung cancer, cervical cancer, ovarian cancer, gastric cancer, metastatic colorectal cancer, malignant lymphoma, etc.

What is the pharmacological action of irinotecan?

Irinotecan powder is a semi-synthetic derivative of camptothecin. It is an inactive prodrug, and its main metabolic site is the liver.

After irinotecan enters the human body through blood, most of it is converted into SN-38(7- ethyl -10- Hydroxycamptothecin) with 100 times of antitumor activity by carboxylesterase (CES), which specifically binds to topoisomerase I(TOP-1), thus achieving the antitumor effect. The other part is transformed into APC and NPC by the CYP3A enzyme in hepatocytes and then transformed into SN-38 by CES to achieve the anti-tumor effect.

Topology isomerase I induce reversible DNA single-strand break, which makes DNA double-strand structure uncoil; Irinotecan and its active metabolite SN-38 can combine with topoisomerase I-DNA complex, thus preventing the reconnection of the broken single strand.

In the process of DNA synthesis, Replicase interacts with the triple complex of topoisomerase I-DNA-CPT-11 and plays a cytotoxic role by causing DNA double-strand breaks. Normally, mammalian cells can't effectively repair this DNA double-strand break.

What are the side effects of irinotecan?

1. Irinotecan, a drug, will have a great impact on the digestive system of patients, so most patients will have nausea, loss of appetite, nausea, indigestion, and other symptoms after taking the drug. Moreover, many patients will have delayed diarrhea, which will lead to abnormal abdominal peristalsis and even death of patients.

2. It may also cause neutropenia in patients, which will lead to the decline of the body's immunity, and may also cause a series of complications. Therefore, in the course of medication, patients should have a regular physical examination and closely monitor various physical indicators to ensure medication safety as much as possible.

3. Irinotecan needs to be metabolized in the liver, so it will cause a great burden on the liver, and may even cause an increase in transaminase, which will have a great impact on liver function. Therefore, for patients with liver diseases or liver dysfunction, it is necessary to use this medicine carefully, otherwise, it is likely to aggravate the condition, which will have a serious impact on health.

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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure or prevent any disease.

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