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Regorafenib

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Regorafenib is an oral multi-kinase inhibitor which targets angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition.

Product Description

Basic Characteristics

Product Name Regorafenib
CAS Number 755037-03-7
Molecular Formula C21H15ClF4N4O3
Formula Weight 482.8
Synonyms Regorafenib;

755037-03-7;

BAY 73-4506;

Stivarga;

4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide.

Appearance White to off-white powder
Storage and Handling Store at room temperature,keep in a cool, dry place, away from direct sunlight.

 

Regorafenib Description

Regorafenib is an oral multi-kinase inhibitor which targets angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition. Since 2009 it was studied as a potential treatment option in multiple tumor types.By 2015 it had two US approvals for advanced cancers.

Regorafenib is a targeted therapy that targets and binds to tyrosine kinase receptors and inhibits epidermal growth factor receptor (EGFR) and vascular endothelial growth factor (VEGF), receptors on the surface of the cell. By binding to these receptors regorafenib blocks an important pathway that promotes cell division.

 

Regorafenib Mechanism of Action

Regorafenib is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment. In in vitro biochemical or cellular assays, regorafenib or its major human active metabolites M-2 and M-5 inhibited the activity of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAFV600E , SAPK2, PTK5, and Abl at concentrations of regorafenib that have been achieved clinically. In in vivo models, regorafenib demonstrated anti-angiogenic activity in a rat tumor model, and inhibition of tumor growth as well as anti-metastatic activity in several mouse xenograft models including some for human colorectal carcinoma.

 

Regorafenib Application

Regorafenib is a targeted cancer drug. You might have it as a treatment for:

▪ Gastro intestinal stromal cancer (GIST) – a rare type of soft tissue sarcoma of the stomach or intestines;

▪ Advanced cancer that started in the liver (primary liver cancer).

 

Regorafenib Side Effects & Warning

We haven’t listed all the side effects. It’s very unlikely that you will have all of these side effects, but you might have some of them at the same time.

How often and how severe the side effects are can vary from person to person. They also depend on what other treatments you’re having. For example, your side effects could be worse if you’re also having other drugs or radiotherapy.

 

Common side effects

▪ Increased risk of getting an infection

▪ Breathlessness and looking pale

▪ Bruising, bleeding gums or nosebleeds

▪ Tiredness and weakness (fatigue)

▪ Soreness, redness and peeling on palms and soles of feet

▪ Loss of appetite and weight loss

▪ Diarrhoea

▪ Voice changes

▪ Voice changes

▪ Mouth sores and ulcers

▪ Skin changes

▪ Feeling or being sick

▪ High levels of bilirubin

▪ High temperature (fever)

 

Reference

[1] “Bayer Announces New Data on Oncology Portfolio To Be Presented at the ECCO-ESMO Congress 2009”. Retrieved 2009-09-19.

[2] “Cancer fund reprieve for just one drug, Regorafenib”. BBC. 22 May 2015. Retrieved 7 June 2015.

[3] FDA Approved Drug Products: STIVARGA (regorafenib) oral tablets

[4] Kim J, Ulu A, Wan D, Yang J, Hammock BD, Weiss RH (May 2016). “Addition of DHA Synergistically Enhances the Efficacy of Regorafenib for Kidney Cancer Therapy”. Molecular Cancer Therapeutics. 15 (5): 890–8.

[5] Hotta K, Ueyama J, Tatsumi Y, Tsukiyama I, Sugiura Y, Saito H, Matsuura K, Hasegawa T: Lack of Contribution of Multidrug Resistance-associated Protein and Organic Anion-transporting Polypeptide to Pharmacokinetics of Regorafenib, a Novel Multi-Kinase Inhibitor, in Rats. Anticancer Res. 2015 Sep;35(9):4681-9.