https://www.aasraw.com/afatinib-on-anti-caners/ https://www.aasraw.com/products/afatinib/ Afatinib powder, sold under the brand name Gilotrif among others, is a medication used to treat non-small cell lung carcinoma (NSCLC).It belongs to the tyrosine kinase inhibitor family of medications.It is taken by mouth.

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6 Questions About Afatinib on
Anti-Caners(NSCLC)
6QuestionsAboutAfatinibonAnti-Caners(NSCLC)............................................................................... 1
WhatIsAfatinib?............................................................................................................................2
WhenWeNeedAfatinib?............................................................................................................. 2
HowDoesAfatinibWork?..............................................................................................................2
WasAfatinibApprovedbyFDA?Sure............................................................................................3
WhatRisk/SideeffectsDoesAfatinibBring?.................................................................................. 4
WhatOtherResearchsAboutAfatinib?.......................................................................................... 5
❶Afatinib(BIBW2992)developmentinnon-small-celllungcancer........................................ 5
❷Afatinibinlocallyadvancedandmetastaticchordoma........................................................ 6
Reference.............................................................................................................................6

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What Is Afatinib?
Afatinib(CAS: 439081-18-2) is a targeted therapy drug that is also known as Giotrif. It is
used to treat non-small cell lung cancer (NSCLC) that has started to spread outside the
lung or to other parts of the body. It may also be used to treat other cancers as part of a
clinical trial.
It is best to read this information with our general information about lung cancer or the
type of cancer you have. Your doctor will talk to you about this treatment and its possible
side effects before you agree (consent) to have treatment. During treatment, you will see
a cancer doctor or nurse. This is who we mean when we mention a doctor or nurse in this
information.
When We Need Afatinib?
Afatinib may be used to treat non-small cell lung cancer (NSCLC) that has:
♦ Spread to surrounding tissues (locally advanced)
♦ Spread to other parts of the body (advanced or metastatic).
Afatinib only works for cancers that have an abnormal form of a protein called epidermal
growth factor receptor (EGFR). Tests are done on the cancer cells from a biopsy or
previous surgery to check the level of EGFR. This tells your doctor whether afatinib is
likely to work for you.
How Does Afatinib Work?
Afatinib is a potent and selective, irreversible ErbB family blocker. Afatinib covalently
binds to and irreversibly blocks signaling from all homo and heterodimers formed by the
ErbB family members EGFR (ErbB1), HER2 (ErbB2), ErbB3 and ErbB4 .
In particular, afatinib covalently binds to the kinase domains of EGFR (ErbB1), HER2
(ErbB2), and HER4 (ErbB4) and irreversibly inhibits tyrosine kinase autophosphorylation,
resulting in downregulation of ErbB signaling. Certain mutations in EGFR, including
non-resistant mutations in its kinase domain, can result in increased autophosphorylation
of the receptor, leading to receptor activation, sometimes in the absence of ligand binding,
and can support cell proliferation in NSCLC. Non-resistant mutations are defined as those

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occurring in exons constituting the kinase domain of EGFR that lead to increased receptor
activation and where efficacy is predicted by 1) clinically meaningful tumor shrinkage with
the recommended dose of afatinib and/or 2) inhibition of cellular proliferation or EGFR
tyrosine kinase phosphorylation at concentrations of afatinib sustainable at the
recommended dosage according to validated methods. The most commonly found of
these mutations are exon 21 L858R substitutions and exon 19 deletions.
Moreover, afatinib demonstrated inhibition of autophosphorylation and/or in vitro
proliferation of cell lines expressing wild-type EGFR and in those expressing selected
EGFR exon 19 deletion mutations, exon 21 L858R mutations, or other less common
non-resistant mutations, at afatinib concentrations achieved in patients. In addition,
afatinib inhibited in vitro proliferation of cell lines overexpressing HER2.
AASraw is the professional manufacturer of
Afatinib.
Was Afatinib Approved by FDA? Sure
Approval provides a new second-line treatment option for patients with the second largest
sub-type of non-small cell lung cancer (NSCLC), representing about 20-30% of NSCLC
cases
Approval is based on results of the LUX-Lung 8 study, which showed significantly
improved overall survival and progression-free survival compared to Tarceva (erlotinib) in
patients with squamous cell carcinoma of the lung
Afatinib is already approved in more than 60 countries for the treatment of patients with
distinct types of EGFR mutation-positive NSCLC

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What Risk/Side
effects Does Afatinib Bring?
Important things to remember about the side effects of afatinib:
▪ Most people will not experience all of the afatinib side effects listed.
▪ Afatinib side effects are often predictable in terms of their onset, duration, and severity.
▪ Afatinib side effects are almost always reversible and will go away after therapy is
complete.
▪ Afatinib side effects may be quite manageable. There are many options to minimize or
prevent the side effects of afatinib.
The following side effects are common (occurring in greater than 30%) for patients
taking afatinib:
▪ Diarrhea
▪ Acneiform eruption (group of skin conditions resembling acne)
▪ Mouth sores
▪ Paronychia (infection of nails)
▪ Dry mouth

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These are less common side effects (occurring in 10-29%) for patients receiving
afatinib:
▪ Decreased appetite
▪ Itching
▪ Weight loss
▪ Nose bleeds
▪ Cystitis (bladder infection)
▪ Cheilitis (inflammation of the lips)
▪ Fever
▪ Hypokalemia (low potassium)
▪ Conjunctivitis (pink eye)
▪ Rhinorrhea (runny nose)
▪ Elevated liver enzymes
Not all side effects are listed above. Some that are rare (occurring in less than about 10
percent of patients) are not listed here. Always inform your health care provider if you
experience any unusual symptoms.
What Other Researchs About Afatinib?
❶Afatinib(BIBW2992)developmentinnon-small-celllungcancer
Afatinib (BIBW 2992), a novel aniline–quinazoline derivative, irreversibly and equipotently
targets the intrinsic kinase activity of all active ErbB receptor family members. Preclinical
results show that afatinib is effective in lung cancer models, including those with EGF
receptor (EGFR) mutations resistant to reversible first-generation EGFR inhibitors.
Afatinib is being investigated in the LUX-Lung program, which will evaluate afatinib as a
first-line treatment in patients with EGFR-activating mutations (LUX-Lung 2, 3 and 6) and
as a second- or third-line treatment in patients that have acquired resistance to gefitinib
and/or erlotinib (LUX-Lung 1, 4 and 5). LUX-Lung 1 and 2 have demonstrated, within their
respective target groups, a significant increase in the disease control rate of 58 and 86%,
respectively, and significant prolongation of progression-free survival. Further Phase III
clinical trials are currently ongoing to assess afatinib in combination with paclitaxel
(LUX-Lung 5), and compared with cisplatin/pemetrexed (LUX-Lung 3) or
cisplatin/gemcitabine (LUX-Lung 6).

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AASraw is the professional manufacturer of
Afatinib.
❷Afatinibinlocallyadvancedandmetastaticchordoma
This is a Phase 2 trial studying the effectiveness of a targeted cancer drug called afatinib.
Afatinib inhibits the EGFR protein, which is believed to be involved in driving the growth of
chordoma tumors. This study is designed specifically for chordoma patients 18 years or
older with recurrent or metastatic tumors. It is currently open at Leiden University Medical
Center (LUMC) and University College London Hospital (UCLH) and will open at Istituto
dei Nazionale Tumori (INT) in Milan in the coming months. The principal investigators for
this study are Dr. Hans Gelderblom at LUMC, Dr. Silvia Stacchiotti at INT, and Dr. Sandra
Strauss at UCLH.
Epidermal Growth Factor Receptor (EGFR) is a protein found on the surface of certain
cells throughout the body. Ordinarily, EGFR helps to regulate cell growth and plays a role
in wound healing. In certain cancers, including most chordomas, EGFR becomes
overactive, leading the cancer cells to multiply out of control.
Drugs that block EGFR called “EGFR inhibitors” are approved to treat several different
types of cancer. Afatinib is an EGFR inhibitor that is currently approved to treat
non-small-cell lung cancer and is being tested in other tumor types.
Several EGFR inhibitors have been shown to slow or stop the growth of chordoma cells
and chordoma tumors in mice. Of all the EGFR inhibitors tested, afatinib was the most
effective in mouse models of chordoma. In some mouse models, it slowed the growth of
the tumors, while in others it caused the tumors to shrink considerably. This trial aims to
determine whether afatinib can shrink or stop the growth of chordoma tumors in patients
with recurrent or metastatic disease.
Reference
[1] Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel Frühjahr 2013. (in German)
[2] Spreitzer H (13 May 2008). “Neue Wirkstoffe – Tovok”. Österreichische
Apothekerzeitung (in German) (10/2008): 498.
[3] Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, et al. (August
2008). “BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung

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cancer models”. Oncogene. 27 (34): 4702–11. doi:10.1038/onc.2008.109. PMC 2748240.
PMID 18408761.
[4] “Giotrif : EPAR -Product Information” (PDF). European Medicines Agency. Boehringer
Ingelheim International GmbH. 16 October 2013. Retrieved 28 January 2014.
[5] Kobayashi Y, Togashi Y, Yatabe Y, Mizuuchi H, Jangchul P, Kondo C, et al.
(December 2015). “EGFR Exon 18 Mutations in Lung Cancer: Molecular Predictors of
Augmented Sensitivity to Afatinib or Neratinib as Compared with First- or
Third-Generation TKIs”. Clinical Cancer Research. 21 (23): 5305–13.
doi:10.1158/1078-0432.CCR-15-1046. PMID 26206867.
[6] Lin NU, Winer EP, Wheatley D, Carey LA, Houston S, Mendelson D, et al. (June 2012).
“A phase II study of afatinib (BIBW 2992), an irreversible ErbB family blocker, in patients
with HER2-positive metastatic breast cancer progressing after trastuzumab”. Breast
Cancer Research and Treatment. 133 (3): 1057–65. doi:10.1007/s10549-012-2003-y.
PMC 3387495. PMID 22418700.