Regorafenib Raw Powder CAS 755037-03-7

Regorafenib (BAY 73-4506) Introduction

Regorafenib (BAY 73-4506) is a small molecule polo kinase inhibitor.Regorafenib Raw Powder appearance is white powder, with CAS number: 755037-03-7; Molecular formula: C21H15ClF4N4O3; Molecular weight: 482.82; EINECS number: 815-051-1. Its molecular structure is similar to Sorafenib. It is a new molecular targeted product developed by Bayer. In September 2012, FDA approved it for the treatment of MCRC patients who have failed to receive multi-line standard treatment. On February 25, 2013, FDA approved it for the treatment of advanced GIST patients who cannot be operated on and other treatment methods are ineffective.

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What is the relationship between regorafenib and rectal cancer?

Colorectal cancer (CRC) is one of the most common gastrointestinal tumors in clinics. Around 1 million 250 thousand people worldwide are diagnosed with CRC each year, and more than 600 thousand patients die, with incidence rate and mortality rate third and fourth respectively. More than 30% of CRC patients have distant metastasis (or mCRC) at the time of diagnosis, and a considerable number of them can not be cured by surgery. The basic products of standardized chemotherapy regimens include 5-Fluorouracil and its derivatives, Oxaliplatin and Irinotecan. However, these cytotoxic products often cause severe side effects, and the traditional chemotherapy often fails to achieve satisfactory results. Regorafenib raw powder is a multi-kinase inhibitor, which targets tumor formation by inhibiting a variety of protein kinases Tumor angiogenesis, and maintenance of tumor microenvironment signal transduction.

What is the pharmacological action of the BAY 73-4506?

Regorafenib raw powder, also known as Fluorosorafenib, is a new multi-target protein kinase inhibitor, which can block tumor cell proliferation, inhibit tumor angiogenesis and regulate the tumor microenvironment. It has good antitumor activity. CORRECT research confirmed that it is a TKI with therapeutic activity for patients with metastatic colorectal cancer. As a new small-molecule tyrosine kinase inhibitor, this product can inhibit multiple tyrosine kinase targets, mainly by inhibiting the activities of VEGFR / VEGFR1, VEGFR2, VEGFR3 tyrosine kinase receptor Tie-2, and platelet-derived growth factor receptor, so as to inhibit angiogenesis.

What is the pharmacokinetics of Regorafenib?

At the interval of 24h administration, several plasma concentration peaks were observed after hepatic intestinal circulation. It was highly bound to human plasma protein (99.5%). Regorafenib Raw Powder was metabolized by cytochrome P450 isoenzyme (CYP3A4) and uridine diphosphate glucosyltransferase (UGT1A9). The main metabolites of regorafenib in human plasma were N-oxide (m-2) and N-oxide and n-demethylate (m-5), Both have similar in vitro pharmacological activities and steady-state concentrations. Both m-2 and m-5 have high protein binding rates (99.8% and 99.95% respectively). After a single-use administration of 160mg of regorafenib, the geometric average elimination half-lives of regorafenib and m-2 in plasma are 28h (14-58h) and 25h (14-32h) respectively. M-5 has a longer average elimination half-life, which is 51h (32-70h). Within 12 days after administration of 120mg of radiolabeled use solution, The excretion of glucuronides is about 17% of the total excretion of glucuronides in the urine.

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FAQ:

Q1:How should regorafenib be used correctly?
The general plan is to have a cycle every 28 days. During the first 21 days of each cycle, 160mg is taken orally every day, followed by a 7-day rest period. Due to individual differences, it is essential to strictly follow the doctor's instructions.
Q2: What are the specific requirements for regorafenib?
It must be swallowed whole after a low-fat meal; take it at the same time every day; if you miss a dose or vomit after taking it, do not make up for it on the same day; continue to take the next dose according to the original plan.
Q3:What is the most common side effect of regorafenib?

The most common adverse reactions include: skin reactions on hands and feet, fatigue, diarrhea, high blood pressure, loss of appetite and infections.

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