Afinitor is used in the treatment of advanced renal cell cancer, after
sunitinib and sorafenib failure. (sunitinib is one of the most
expensive drugs widely marketed)
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Full text
Generic Name: Everolimus
Afinitor is the trade name for the generic name drug everolimus. In
some cases, health care professionals may use the generic name
everolimus when referring to the trade drug name Afinitor.
Drug Type:
Afinitor is a targeted therapy and is classified as an mTOR inhibitor.
What Afinitor Is Used For:
Afinitor is used in the treatment of advanced renal cell cancer, after
sunitinib (see below) and sorafenib failure.
Note: If a drug has been approved for one use, physicians may elect to
use this same drug for other problems if they believe it may be
helpful.
How Afinitor Is Given:
Afinitor is given as a tablet by mouth.
Take at the same time each day, may be taken with or without food.
Swallow whole with a glass of water, do not chew or crush tablets.
Avoid contact with or exposure to crushed or broken tablets.
There are 2 tablet strengths
5mg tablet; white to slightly yellow, elongated tablet with a
bevelled edge and no score, engraved with "5" on one side and "NVR" on
the other
10mg tablet; white to slightly yellow, elongated tablet with a
bevelled edge and no score, engraved with "UHE" on one side and "NVR"
on the other.
The amount of Afinitor that you will receive will be prescribed by
your doctor based on established dosing guidelines.
Afinitor Side effects:
Important things to remember about the side effects of Afinitor:
You will not get all of the Afinitor side effects mentioned below.
Afinitor side effects are often predictable in terms of their
onset, duration, and severity.
Afinitor side effects are almost always reversible and will go
away after therapy is complete.
Afinitor side effects are quite manageable. There are many options
to minimize or prevent them.
The following side effects are common (occurring in greater than 30%)
for patients taking Afinitor:
Low red blood cell count(anemia)
Increased blood cholesterol level
Increased blood trigylceride level
Increased creatinine
Mouth sores
low phosphorus level
Infection
Weakness
Diarrhea
Cough
These are less common (occurring in 10-29%) side effects for patients
receiving everolimus:
Rash
Low blood counts. Your white blood cells and platelets may
temporarily decrease. This can put you at increased risk for
infectionand/or bleeding.
Nausea, vomiting
Increased liver enzymes
Swelling
Poor appetite
Shortness of breath
Fever
Fatigue
Headache
Nosebleeds
Itching
Lung problems
Dry skin
This list includes common and less common side effects for those
taking Afinitor. Side effects that are very rare -- occurring in less
than about 10 percent of patients -- are not listed here. But you
should always inform your health care provider if you experience any
unusual symptoms.
When To Contact Your Doctor or Health Care Provider:
Contact your health care provider immediately, day or night, if you
should experience any of the following symptoms:
Fever of 100.5º F (38º C) or higher, chills (possible signs of infection)
The following symptoms require medical attention, but are not an
emergency. Contact your health care provider within 24 hours of
noticing any of the following:
Nausea (interferes with ability to eat and unrelieved with
prescribed medication)
Vomiting (vomiting more than 4-5 times in a 24 hour period)
Diarrhea (4-6 episodes in a 24-hour period)
Unusual bleeding or bruising
Black or tarry stools, or blood in your stools
Blood in the urine
Pain or burning with urination
Extreme fatigue (unable to carry on self-care activities)
Mouth sores (painful redness, swelling or ulcers)
Always inform your health care provider if you experience any unusual symptoms.
Precautions While Taking Afinitor:
Before starting Afinitor treatment, make sure you tell your doctor
about any other medications you are taking (including prescription,
over-the-counter, vitamins, herbal remedies, etc.).
Do not receive any kind of immunization or vaccination without
your doctor's approval while taking Afinitor.
Inform your health care professional if you are pregnant or may be
pregnant prior to starting this treatment. Pregnancy category D
(Afinitor may be hazardous to the fetus. Women who are pregnant or
become pregnant must be advised of the potential hazard to the fetus.)
For both men and women: Do not conceive a child (get pregnant)
while taking Afinitor. Barrier methods of contraception, such as
condoms, are recommended. Discuss with your doctor when you may safely
become pregnant or conceive a child after therapy.
Do not breast feed while taking this medication.
Self-care Tips While Taking Afinitor:
Drink at least two to three quarts of fluid every 24 hours, unless
you are instructed otherwise.
You may be at risk of infection so try to avoid crowds or people
with colds, and report fever or any other signs of infection
immediately to your health care provider.
Wash your hands often.
To help treat/prevent mouth sores, use a soft toothbrush, and
rinse three times a day with 1 teaspoon of baking soda mixed with 8
ounces of water.
Use an electric razor and a soft toothbrush to minimize bleeding.
Avoid contact sports or activities that could cause injury.
To reduce nausea, take anti-nausea medications as prescribed by
your doctor, and eat small, frequent meals.
Avoid sun exposure. Wear SPF 15 (or higher) sunblock and
protective clothing.
In general, drinking alcoholic beverages should be kept to a
minimum or avoided completely. You should discuss this with your
doctor.
Get plenty of rest.
Maintain good nutrition.
If you experience symptoms or side effects, be sure to discuss
them with your health care team. They can prescribe medications and/or
offer other suggestions that are effective in managing such problems.
Monitoring and Testing While Taking Afinitor:
You will be checked regularly by your doctor while you are taking
Afinitor, to monitor side effects and check your response to therapy.
Periodic blood work will be obtained to monitor your complete blood
count (CBC) as well as the function of other organs (such as your
kidneys and liver) will also be ordered by your doctor.
How Afinitor Works:
Targeted therapy is the result of about 100 years of research
dedicated to understanding the differences between cancer cells and
normal cells. To date, cancer treatment has focused primarily on
killing rapidly dividing cells because one feature of cancer cells is
that they divide rapidly. Unfortunately, some of our normal cells
divide rapidly too, causing multiple side effects.
Targeted therapy is about identifying other features of cancer cells.
Scientists look for specific differences in the cancer cells and the
normal cells. This information is used to create a targeted therapy
to attack the cancer cells without damaging the normal cells, thus
leading to fewer side effects. Each type of targeted therapy works a
little bit differently but all interfere with the ability of the
cancer cell to grow, divide, repair and/or communicate with other
cells.
There are different types of targeted therapies, defined in three
broad categories. Some targeted therapies focus on the internal
components and function of the cancer cell. The targeted therapies
use small molecules that can get into the cell and disrupt the
function of the cells, causing them to die. There are several types
of targeted therapy that focus on the inner parts of the cells.
Other targeted therapies target receptors that are on the outside of
the cell. Antiangiogenesis inhibitors target the blood vessels that
supply oxygen to the cells, ultimately causing the cells to starve.
Researchers agree that targeted therapies are not a replacement for
traditional therapies. They may best be used in combination with
traditional therapies. More research is needed to identify which
cancers may be best treated with targeted therapies and to identify
additional targets for more types of cancer.
Afinitor is an inhibitor of mTOR. mTOR inibition blocks the
translation of genes that regulate cancer cell proliferation. It also
results in reduced levels of certain cell growth factors involved in
the development of new blood vessels, such as vascular endothelial
growth factor (VEGF).
Note: We strongly encourage you to talk with your health care
professional about your specific medical condition and treatments. The
information contained in this website is meant to be helpful and
educational, but is not a substitute for medical advice.
SUNITINIB
is one of the most expensive drugs widely marketed.
Doctors and editorials have criticized the high cost, for a drug that
doesn't cure cancer but only prolongs life.
Sunitinib (marketed as Sutent by Pfizer, and previously known as
SU11248) is an oral, small-molecule, multi-targeted receptor tyrosine
kinase (RTK) inhibitor that was approved by the FDA for the treatment
of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal
stromal tumor (GIST) on January 26, 2006. Sunitinib was the first
cancer drug simultaneously approved for two different indications
Renal cell carcinoma
Sunitinib is approved for treatment of metastatic RCC. Other
therapeutic options in this setting are sorafenib (Nexavar),
temsirolimus (Torisel), interleukin-2 (Proleukin), everolimus
(Affinitor), and bevacizumab (Avastin).
RCC is generally resistant to chemotherapy or radiation. Prior to
RTKs, metastatic disease could only be treated with the cytokines
interferon alpha (IFNα) or Interleukin 2 (IL-2). However, these agents
demonstrated low rates of efficacy (5%-20%).
In a phase 3 study, median progression-free survival was significantly
longer in the sunitinib group (11 months) than in the interferon alfa
group (5 months), hazard ratio 0.42.[6][11] In the secondary
endpoints, 28% of had significant tumor shrinkage with sunitinib
compared to 5% with IFNα. Patients receiving sunitinib had a better
quality of life than IFNα.
At ASCO 2008, Dr Robert Figlin presented updated data from the final
study analysis, including overall survival. The primary endpoint of
median progression-free survival (PFS) remained superior with
sunitinib: 11 months versus 5 months for IFNα, P<.000001. Objective
response rate also remained superior: 39-47% for sunitinib versus
8-12% with IFNα, P<.000001.[12][13]
Sunitinib was associated with somewhat longer overall survival,
although this was not statistically significant.
Median OS was 26 months with sunitinib vs 22 months for IFNα
regardless of stratification (P-value ranges from .051 to .0132,
depending on statistical analysis).
The first analysis includes 25 patients initially randomized to
IFNα who crossed over to sunitinib therapy, which may have confounded
the results; in an exploratory analysis that excluded these patients,
the difference becomes more robust: 26 vs 20 months, P=.0081.
Patients in the study were allowed to receive other therapies once
they had progressed on their study treatment. For a "pure" analysis of
the difference between the two agents, an analysis was done using only
patients who did not receive any post-study treatment. This analysis
demonstrated the greatest advantage for sunitinib: 28 months vs 14
months for IFNα, P=.0033. The number of patients in this analysis was
small and this does not reflect actual clinical practice and is
therefore not meaningful.
Also worth noting in this presentation was the fact that the
updated percentage of patients that had to discontinue sunitinib due
to adverse events was 19%. This is a clinically meaningful number.
This was the largest comparative trial in RCC to date, and sunitinib
is the first agent to demonstrate an overall survival longer than 2
years in these patients.
Hypertension was found to be a biomarker of efficacy in patients with
metastatic renal cell carcinoma treated with sunitinib.[14] Patients
with mRCC and sunitinib-induced hypertension had better outcomes than
those without treatment-induced HTN (objective response rate: 54.8% vs
8.7%; median PFS: 12.5 months, 95% confidence interval [CI] = 10.9 to
13.7 vs 2.5 months, 95% CI = 2.3 to 3.8 months; and OS: 30.9 months,
95% CI = 27.9 to 33.7 vs 7.2 months, 95% CI = 5.6 to 10.7 months; P <
.001 for all).
[edit] Other solid tumors
The efficacy of sunitinib is currently being evaluated in a broad
range of solid tumors, including breast, lung, thyroid and colorectal
cancers. Early studies have shown single-agent efficacy in a number of
different areas. Sunitinib blocks the tyrosine kinase activities of
KIT, PDGFR, VEGFR2 and other tyrosine kinases that are involved in the
development of tumours.
A Phase II study in previously-treated patients with metastatic
breast cancer found that sunitinib "has significant single agent
activity" [15]
A Phase II study of refractory non-small-cell lung cancer found
that "Sunitinib has provocative single-agent activity in previously
treated pts with recurrent and advanced NSCLC, with the level of
activity similar to currently approved agents." [16]
In a Phase II study of patients with nonresectable neuroendocrine
tumors (NET), 91% of patients responded to sunitinib (9% partial
response + 82% stable disease) [17]
Unsuccessful trials
Between April 2009 and May 2011 Pfizer has reported unsuccessful
late-stage trials in breast cancer, metastatic colorectal cancer,
advanced non-small-cell lung cancer, and castration-resistant prostate
cancer.[18]
History
The drug was discovered at SUGEN a biotechnology company which
pioneered protein kinase inhibitors. It was the third in a series of
compounds including SU5416 (Semaxanib) and SU6668. The concept was of
a ATP analogue that would compete with ATP for binding to the
catalytic site of receptor tyrosine kinases.[citation needed] This
concept led to the invention of many small-molecule tyrosine kinase
inhibitors including Gleevec, Sutent, Tarceva and many other cancer
drugs.
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