Luhan Pharmachem Co., Ltd.

Luhan pharmachem Co., Ltd. supplies Crizotinib bulk active pharmaceutical ingredient (API) to the pharmaceutical industry. Our Crizotinib is manufactured by cGMP compliant facility. Welcome to contact us for further details including current DMF status for the product and up to date regulatory status of the manufacturing facility. We look forward to assisting you with your research and development projects.

What is Crizotinib?

Crizotinib (trade name Xalkori, case Pfizer), is an anti-cancer drug acting as an ALK (anaplastic lymphoma kinase) and ROS1 (c-ros oncogene 1) inhibitor, approved for treatment of some non-small cell lung carcinoma (NSCLC) in the US and some other countries, and undergoing clinical trials testing its safety and efficacy in anaplastic large cell lymphoma, neuroblastoma, and other advanced solid tumors in both adults and children.

Indications

Crizotinib is a prescription medicine used to treat non-small cell lung cancer (NSCLC) that is advanced or has spread to other parts of the body and is caused by a defect in a gene called ALK (anaplastic lymphoma kinase). Crizotinib approval is based on the percentage of patients whose tumors responded to treatment.

Mechanism of Action

Crizotinib has an aminopyridine structure, and functions as a protein kinase inhibitor by competitive binding within the ATP-binding pocket of target kinases. About 4% of patients with non-small cell lung carcinoma have a chromosomal rearrangement that generates a fusion gene between EML4 (‘echinoderm microtubule-associated protein-like 4’) and ALK (‘anaplastic lymphoma kinase’), which results in constitutive kinase activity that contributes to carcinogenesis and seems to drive the malignantphenotype. The kinase activity of the fusion protein is also inhibited by crizotinib. Patients with this gene fusion are typically younger non-smokers who do not have mutations in either the epidermal growth factor receptor gene (EGFR) or in the K-Ras gene. The number of new cases of ALK-fusion NSLC is about 9,000 per year in the U.S. and about 45,000 worldwide.

ALK mutations are also thought to be important in driving the malignant phenotype in about 15% of cases of neuroblastoma, a rare form of peripheral nervous system cancer that occurs almost exclusively in very young children.

Crizotinib also inhibits the c-Met/Hepatocyte growth factor receptor (HGFR) tyrosine kinase, which is involved in the oncogenesis of a number of other histologicalforms of malignant neoplasms.

Crizotinib is currently thought to exert its effects through modulation of the growth, migration, and invasion of malignant cells. Other studies suggest that Crizotinib may also act via inhibition of angiogenesis in malignant tumors.

What are the side effects of Crizotinib?

Common side effects of Crizotinib include:

• vision problems: these problems usually happen within 2 weeks of starting Crizotinib. Tell your doctor right away if you have any change in vision, such as: flashes of light, blurred vision, light hurting your eyes, or new or increased floaters
• nausea
• diarrhea
• vomiting
• swelling of your hands or feet
• constipation

Precautions

Before you take Crizotinib, tell your doctor if you:

• have heart problems, including a condition called long QT syndrome
• have liver or kidney problems
• have any other medical conditions
• are pregnant, or plan to become pregnant. Crizotinib may harm your unborn baby.

Women who are able to become pregnant and men who take Crizotinib should use birth control during treatment and for 3 months after stopping Crizotinib.

Talk to your doctor about the birth control methods that may be right for you.

Storage

Store Crizotinib at room temperature (20 to 25 degrees Celsius).

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.