https://www.aasraw.com/products/erlotinib/ https://www.aasraw.com/using-erlotinib/ Erlotinib Powder, sold under the brand name Tarceva among others, is a medication used to treat non-small cell lung cancer (NSCLC) and pancreatic cancer. Specifically it is used for NSCLC with mutations in the epidermal growth factor receptor (EGFR) — either an exon 19 deletion (del19) or exon 21 (L858R) substitution mutation — which has spread to other parts of the body. #Erlotinib,

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What is Erlotinib?
Basic Characteristics
Product Name Erlotinib powder
CAS Number 183321-74-6
Molecular
Formula
C22H23N3O4
Formula Weight 393.443
Synonyms
CP-358774;
OSI774;
Erlotinib powder free base;
183321-74-6.
Appearance White to off-white crystalline powder
Storage and
Handling
Dry, dark and at 0 – 4 C for short term (days to weeks) or
-20 C for long term (months to years).
Erlotinib Powder Description
Erlotinib powder, sold under the brand name Tarceva among others,
is a medication used to treat non-small cell lung cancer (NSCLC) and
pancreatic cancer. Specifically it is used for NSCLC with mutations in
the epidermal growth factor receptor (EGFR) — either an exon 19
deletion (del19) or exon 21 (L858R) substitution mutation — which
has spread to other parts of the body. It is taken by mouth.

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Erlotinib powder is a quinazoline derivative with antineoplastic
properties. Competing with adenosine triphosphate, erlotinib powder
reversibly binds to the intracellular catalytic domain of epidermal
growth factor receptor (EGFR) tyrosine kinase, thereby reversibly
inhibiting EGFR phosphorylation and blocking the signal transduction
events and tumorigenic effects associated with EGFR activation.
Erlotinib powder was approved for medical use in the United States in
2004. It is on the World Health Organization’s List of Essential
Medicines, which lists the safest and most effective medicines
needed in a health system.
Erlotinib Powder Mechanism of Action
Erlotinib powder is an epidermal growth factor receptor inhibitor
(EGFR inhibitor). The drug follows Iressa (gefitinib), which was the
first drug of this type.
Erlotinib powder specifically targets the epidermal growth factor
receptor (EGFR) tyrosine kinase, which is highly expressed and
occasionally mutated in various forms of cancer. It binds in a
reversible fashion to the adenosine triphosphate (ATP) binding site of
the receptor. For the signal to be transmitted, two EGFR molecules
need to come together to form a homodimer.
These then use the molecule of ATP to trans-phosphorylate each
other on tyrosine residues, which generates phosphotyrosine
residues, recruiting the phosphotyrosine-binding proteins to EGFR to
assemble protein complexes that transduce signal cascades to the
nucleus or activate other cellular biochemical processes. When
erlotinib powder binds to EGFR, formation of phosphotyrosine
residues in EGFR is not possible and the signal cascades are not
initiated.
Erlotinib powder also is a tyrosine kinase receptor inhibitor that is
used in the therapy of advanced or metastatic pancreatic or non-small

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cell lung cancer. Erlotinib powder therapy is associated with transient
elevations in serum aminotransferase levels during therapy and rare
instances of clinically apparent acute liver injury.
Erlotinib Powder Application
Erlotinib powder is a reversible first-generation receptor tyrosine
kinase inhibitor (along with Gefitinib) acting primarily on the epidermal
growth factor receptor (EGFR), a member of the ErbB receptor family.
The drug interacts with both wild type and mutation EGFR. The ErbB
family can form homodimers or heterodimers, which are often
implicated in downstream effects and pathogenesis of many types of
carcinomas studied in humans. Receptor tyrosine kinase inhibitors
(TKI) prevent the phosphorylation of their substrate in the cell
signaling pathway. EGFR normally plays a role in many cellular
functions, including differentiation, proliferation, and angiogenesis, all
of which are hallmarks of cancer.
EGFR mutation in NSCLC is typically an activating mutation. Some
patient characteristics that make the presence of EGFR mutation
more likely include no history of smoking confirmed adenocarcinoma
by histologic analysis, Asian ethnicity, and female sex. Secondary
mutations in the EGFR commonly occur, which this article describes
below.
Erlotinib Powder Side Effects & Warning
The following side effects are common for patients taking Erlotinib
Powder:
Rash
Diarrhea
Poor appetite

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Fatigue
Shortness of breath
Cough
Nausea and vomiting
These side effects are less common side effects of patients receiving
Erlotinib Powder:
Infection
Mouth sores
Itching
Dry skin
Eye irritation
Abdominal pain
Not all side effects are listed above. Some that are rare (occurring in
less than 10% of patients) are not listed here. However, you should
always inform your health care provider if you experience any unusual
symptoms.
Reference
[1] Gao JW, Zhan P, Qiu XY, Jin JJ, Lv TF, Song Y. Erlotinib-based
doublet targeted therapy versus erlotinib powder alone in previously
treated advanced non-small-cell lung cancer: a meta-analysis from 24

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randomized controlled trials. Oncotarget. 2017 May
31;8(42):73258-73270. doi: 10.18632/oncotarget.18319. eCollection
2017 Sep 22. Review. PubMed PMID: 29069867; PubMed Central
PMCID: PMC5641210.
[2] Lee CK, Davies L, Wu YL, Mitsudomi T, Inoue A, Rosell R, Zhou C,
Nakagawa K, Thongprasert S, Fukuoka M, Lord S, Marschner I, Tu
YK, Gralla RJ, Gebski V, Mok T, Yang JC. Gefitinib or Erlotinib
powder vs Chemotherapy for EGFR Mutation-Positive Lung Cancer:
Individual Patient Data Meta-Analysis of Overall Survival. J Natl
Cancer Inst. 2017 Jun 1;109(6). doi: 10.1093/jnci/djw279. Review.
PubMed PMID: 28376144.
[3] Yang Z, Hackshaw A, Feng Q, Fu X, Zhang Y, Mao C, Tang J.
Comparison of gefitinib, erlotinib powder and afatinib in non-small cell
lung cancer: A meta-analysis. Int J Cancer. 2017 Jun
15;140(12):2805-2819. doi: 10.1002/ijc.30691. Epub 2017 Mar 27.
Review. PubMed PMID: 28295308.
[4] “Erlotinib powder (Tarceva) Use During Pregnancy”. Drugs.com. 1
November 2019. Retrieved 23 December 2019.
[5] “Erlotinib powder Monograph for Professionals”. Drugs.com.
Retrieved 12 November 2019.
[6] “Tarceva- erlotinib powder hydrochloride tablet”. DailyMed. 12
December 2018. Retrieved 23 December 2019.
[7] “Drug Approval Package: Tarceva (Erlotinib powder) NDA
#021743”. U.S. Food and Drug Administration (FDA). 28 March 2005.
Retrieved 23 December 2019.
[8] Raymond E, Faivre S, Armand JP (2000). “Epidermal growth factor
receptor tyrosine kinase as a target for anticancer therapy”. Drugs. 60
Suppl 1: 15–23, discussion 41–2.
doi:10.2165/00003495-200060001-00002. PMID 11129168. S2CID
10555942.

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