Showing posts with label tyrosine kinase. Show all posts
Showing posts with label tyrosine kinase. Show all posts

Saturday, March 14, 2020

Chemotherapy and Its Side Effects: Chapter 3 - Side Effects of Chemotherapy

D. Other Side Effects


D.1. Liver damage

Liver is a vital organ and has a wide range of functions. Liver produces bile to aid in digestion through the emulsification of lipids and plays a major role in metabolism. Other functions of liver include hormone production, decomposition of red blood cells (RBCs), plasma protein synthesis, and detoxification of small and complex molecules.

Theoretically, all drugs are associated with certain toxicity (but to different extents) and liver is the major organ that is supposed to “detoxify” the drugs mainly by breaking down the drugs into metabolite(s). The other way for liver to make a drug less toxic is to make it more water soluble, thus more easily excreted out of the body and reduce potential toxicity. However, a small percentage of drugs are able to evade the “protection mechanism” by the liver. In this case, the drugs pass through the body’s major detoxifying guard (liver), damage liver, and move to other organs to exert other side effects.


A typical example of anticancer drugs with potential liver toxicity is cisplatin. Tyrosine kinase inhibitors are also associated with potential liver toxicity. Recently, the FDA required a “black box warnings” to be included on labels of several anticancer drugs to indicate the increased risk of liver injury including some tyrosine kinase inhibitors.


© Jiajiu Shaw, 2020

Disclaimer: This blog is written solely for informational purposes. It does not constitute the practice of any medical, nursing or other medical professional health care advice, diagnosis, or treatment. All contents posted are extracted from the book, "SIDE EFFECTS OF CHEMOTHERAPY AND RADIOTHERAPY", prepared by Dr. Jiajiu Shaw, Dr. Frederick Valeriote, and Dr. Ben Chen.

Saturday, May 18, 2019

Chemotherapy and Its Side Effects: Chapter 2 - Kinase Modulators (cont'd)

E.2. Afatinib (Gilotrif™, Giotrif®)

The commercial product of afatinib (Fig. 1.13) is an orally administered inhibitor of the ErbB family of tyrosine kinases. Afatinib also inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR). The inhibition is through the formation of a C-S covalent bond between afatinib and a cysteine in EGFR.


Fig. 1.13  Afatinib

Afatinib (Fig. 1.13) was first indicated for treating non-small cell lung cancer. In addition, it has been reported that afatinib may be useful to treat other cancers.

© Jiajiu Shaw, 2019

Disclaimer: This blog is written solely for informational purposes. It does not constitute the practice of any medical, nursing or other medical professional health care advice, diagnosis, or treatment. All contents posted are extracted from the book, "SIDE EFFECTS OF CHEMOTHERAPY AND RADIOTHERAPY", prepared by Dr. Jiajiu Shaw, Dr. Frederick Valeriote, and Dr. Ben Chen. 

Saturday, March 30, 2019

Chemotherapy and Its Side Effects: Chapter 2 - Kinase Modulators (cont'd)


E.1. Imatinib mesylate (sold as Gleevec® by Novartis)


Fig. 1.12

Imatinib (Fig. 1.12) was first approved by the FDA in 2001 and sold as Gleevec®. It works by specifically targeting, and turning off constitutively active tyrosine kinases (Bcr-abl) which help cancer cells grow and multiply. Bcr-abl kinase is a hybrid product of a chimeric Bcr-abl oncogene caused by translocation between chromosomes 9 and 22. The tyrosine kinases cause several cancers including Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) and gastrointestinal stromal tumor (GIST). Gleevac comes in tablet form. When given by oral administration, the active ingredient, imatinib, is rapidly absorbed.

Potential side effects of Gleevec include fluid retention, rash, nausea & vomiting, muscle cramps, and diarrhea. 

© Jiajiu Shaw, 2019

Disclaimer: This blog is written solely for informational purposes. It does not constitute the practice of any medical, nursing or other medical professional health care advice, diagnosis, or treatment. All contents posted are extracted from the book, "SIDE EFFECTS OF CHEMOTHERAPY AND RADIOTHERAPY", prepared by Dr. Jiajiu Shaw, Dr. Frederick Valeriote, and Dr. Ben Chen. 

Saturday, November 19, 2016

Natural Products for Cancer Prevention/Management (9)

Quercetin

Quercetin is a representative flavonoid found in many plants including citrus fruit, tea, onion, and apples. Quercetin has been made in capsule form as a dietary supplement for quite some time. It has been shown to have several beneficial biological/pharmaceutical effects, including antioxidant, anti-inflammatory, and anticancer.

Most of the research on quercetin and cancer has been done in cell culture (in vitro studies) or animal studies (in vivo studies). One must be cautious that these studies are not equivalent to human clinical trials. In vitro studies indicate that quercetin can slow the growth of some cancer cells. Clinical studies indicate its involvement in tyrosine kinase inhibition but there is no solid clinical evidence indicating that quercetin can prevent or treat cancer.


Some studies suggested potential protective value for quercetin in prostatitis (inflamed prostate), heart disease, and cancer. However, it is not clear what role quercetin played in their findings. All these sound exciting; however, further clinical studies are needed before any scientific conclusions can be made. Nevertheless, it is not a bad idea to include foods that contain quercetin as part of a balanced diet with an emphasis on fruits, vegetables, legumes, and whole grains.

© Jiajiu Shaw, 2016

Disclaimer: This blog is written solely for informational purposes. It does not constitute the practice of any medical, nursing or other medical professional health care advice, diagnosis, or treatment. All contents posted are extracted from the book I am writing, "IS CANCER IN US", to be published in about two months.