What are multikinase inhibitors?

What are multikinase inhibitors?

What are Multikinase inhibitors? Multikinase inhibitors work by inhibiting multiple intracellular and cell surface kinases, some of which are implicated in tumor growth and metastatic progression of cancer, thus decreasing tumor growth and replication.

What are the side effects of regorafenib?

Regorafenib may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

• tiredness.
• weakness.
• loss of appetite.
• diarrhea.
• swelling, pain, and redness of the lining of your mouth or throat.
• weight loss.
• hoarseness or other change in the sound of your voice.

What does regorafenib target?

Regorafenib (BAY 73-4506, Stivarga®) is an oral diphenylurea multi-kinase inhibitor that targets angiogenic (VEGFR1-3, TIE2), stromal (PDGFR-β, FGFR), and oncogenic receptor tyrosine kinases (KIT, RET, and RAF).

Is regorafenib cytotoxic?

With this in mind, we used the Chou-Talalay median effects analysis to demonstrate that the combination of regorafenib with a PKD inhibitor resulted in a significant synergistic cytotoxic effect in CRC cells that expressed different genetic mutation profiles.

What is a protein kinase inhibitor used for?

Blocking certain protein kinases may help keep cancer cells from growing. Some protein kinase inhibitors, such as imatinib, vemurafenib, and gefitinib, are used to treat cancer.

Who makes sunitinib?

Sunitinib is marketed by Pfizer as Sutent, and is subject to patents and market exclusivity as a new chemical entity until February 15, 2021.

Is regorafenib an immunotherapy?

Regorafenib may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth. Immunotherapy with monoclonal antibodies, such as ipilimumab and nivolumab, may help the body’s immune system attack the cancer, and may interfere with the ability of tumor cells to grow and spread.

How do you take sildenafil citrate 50mg tablets?

You have been prescribed Sildenafil Citrate 50mg Tablet for the treatment of erectile dysfunction. It is best to take it an hour before sexual intercourse. But, you can take it anytime between 30 minutes and 4 hours before sexual activity. Do not take it more than once a day.

Does stivarga shrink tumors?

Regorafenib (Stivarga) Regorafenib can slow tumor growth and even shrink some tumors, although it’s not clear if it can help people live longer. Common side effects of regorafenib include belly pain, diarrhea, feeling tired or weak, mouth or throat irritation, fever, loss of appetite, and weight loss.

What is the cost of regorafenib?

And those 0.04 QALYs proved costly. Including adverse events, the price of regorafenib equaled $39,391 for the total treatment duration. “In all 1-way sensitivity analyses,” noted Dr Goldstein, “the ICER of regorafenib was greater than $700,000 per QALY.

Is a kinase inhibitor chemotherapy?

Any drug used to treat cancer (including tyrosine kinase inhibitors or TKIs) can be considered chemo, but here chemo is used to mean treatment with conventional cytotoxic (cell-killing) drugs that mainly kill cells that are growing and dividing rapidly.

What type of drugs are kinase inhibitors?

To date, many Type I kinase inhibitors for the treatment of cancer have been approved by the FDA viz. bosutinib, crizotinib, dasatinib, erlotinib, gefitinib, lapatinib, pazopanib, ruxolitinib, sunitinib, and vemurafenib.

What kind of kinase is regorafenib an inhibitor of?

Regorafenib is an inhibitor of stromal, angiogenic, and oncogenic receptor tyrosine kinases, as well as the RAF/MEK/ERK signaling pathway.

What is the antiangiogenic effect of regorafenib?

Furthermore, regorafenib inhibits additional angiogenic kinases (VEGFR1/3, platelet-derived growth factor receptor-β and fibroblast growth factor receptor 1) and the mutant oncogenic kinases KIT, RET and B-RAF. The antiangiogenic effect of regorafenib was demonstrated in vivo by dynamic contrast-enhanced magnetic resonance imaging.

What are the side effects of regorafenib in GISTs?

The most commonly observed grade ≥3 AEs included hypertension, hand-foot skin reaction, rash, diarrhea, and fatigue. Conclusions: Regorafenib is a novel oral multikinase inhibitor that has shown promising results for patients with advanced, unresectable or metastatic treatment-refractory CRCs or imatinib- and sunitinib-resistant GISTs.

What are the results of the regorafenib MCRC trial?

Phase III CORRECT (Regorafenib Monotherapy for Previously Treated Metastatic Colorectal Cancer) trial data demonstrated an overall survival benefit for mCRC patients treated with regorafenib (6.4 vs 5.0 months; P = .0052).