Title: Sorafenib - Mechanism of Action in treating Advanced Hepatocellular Carcinoma
1Sorafenib - Mechanism of Action in treating
Advanced Hepatocellular Carcinoma
2Hepatocellular Carcinoma or HCC is the most
common type of liver cancer and is responsible
for over 90 of liver cancer deaths. It is
estimated that 600,000 new cases of HCC are
diagnosed annually which amounts to about 5 of
all the cancer cases. The estimated survival
time for HCC is 4 to 6 months as it carries a
very poor prognosis. Chemotherapeutic agents have
not yet shown any successful results in patients.
3Sorafenib / Nexavar is approved by the FDA for
the treatment of renal cell carcinoma. As a
result of recent trials in treating solid tumours
like HCC. Sorafenib is found to have positive
effects in expanding the survival time of HCC
patients. Sorafenib / Nexavar is a multikinase
inhibitor. Sorafenib when combined with the
conventional transarterial chemoembolization
improved time for progression, tumour response
rate and progression-free survival when compared
to treatment with Sorafenib alone.
4Sorafenib / Nexavar Cost Information Sorafenib /
Nexavar Usage Sorafenib tosylate is identifiable
through the serial modification of the commercial
Raf kinase inhibitor. It works by inhibiting or
blocking the pathways that involves the proteins
that enable tumour growth. Some of these
functions have been proven successful through
clinical trials while some functions are still
are under consideration for confirmation.
5Sorafenib is generally taken as an oral tablet
twice in a day. It is primarily metabolized in
the liver through oxidative metabolism by
cytochrome p450 or by glucuronidation mediated by
UGT1A9. In patients with chronic liver disease,
the metabolism is not altered. Dose adjustments
are required due to factors such as body weight,
age, gender and mild-moderate hepatic or renal
impairment. Sorafenib tablets comes in the doses
of Brand Nexavar 200 mg tablets.
6Sorafenib / Nexavar Price Information Sorafenib
Mechanism of Action Sorafenib / Nexavar inhibits
many kinases that are involved in tumour cell
growth and its blood supply. These
include Raf Raf is a serine / theoine kinase
which when activated by localized membrane
protein called Ras enables gene transcription in
the nucleus. This leads to several tumour
promoting effects.
7VEGFR VEGR is the main mediator of normal as
well as tumour related angiogenesis. It enables
this effect through several functions like
induction of endothelial cell division
migration, reversal of endothelial cell aging and
the promotion of endothelial cell survival. It
interacts with VEGFR which is found on the
endothelial cells surface. This leads to a
several downstream proteins to be activated and
autophosphorylation of intra-cellular receptor
tyrosine kinase.
8- PDGFR
- PDGF interacts with receptor capillary
endothelial cells surface. The interaction of
PDGF to the receptors causes several changes on
the endothelial cell motility and apoptosis. - Sorafenib / Nexavar Side Effects
- Sorafenib side effects include
- Easy and unusual bruises, heavy menstrual
periods, on-going bleeding. - Bloody urine or stool, coughing and vomiting
blood - Dry coughs and wheezing
- Mouth sores
9- Pain in upper stomach, loss of appetite,
itchiness, jaundice and/or dark urine - Chest pains, fainting and dizziness, swellings,
sweating, shortness of breath and/or rapid weight
gain - Rapid heartbeats, pale skin, trouble in focusing,
light-headedness - High blood pressure, signs severe headache,
buzzing in ears, uneven heartbeats, seizure,
confusion, blurred vision - Rashes and severe pain in soles of the feet and
palms of the hand - Skin reactions, signs swelled face or tongue,
burning sensation in the eyes, skin pains
followed by a red or purple skin rash (may lead
to blistering and peeling of the skin), fever
and/or sore throat
10- Some of the more common side effects include
- Mild itching and rashes
- Weight loss and thinning hair
- Tiredness
- Vomiting, mild stomach pains and diarrhoea
- Sorafenib Cost Information
- The information provided on the page is meant for
the purpose of being helpful and educational. It
should not be considered as medical advice.
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