Erlotinib Hydrochloride

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Cat Number

API183319699

CAS Number

183319-69-9

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CAS Number

183319-69-9

EINECS

620-491-0

Storage

Store at room temperature

Synonyms

erlotinib HCl; Tarceva; OSI-774; CP 358774; DA87705X9K; CP-358

Molecular Formula

C22H24ClN3O4

Molecular Weight

429.9

Smiles

COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl

Appearance

White to off-white powder

General Description

Erlotinib hydrochloride is a small-molecule tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR). It is available as oral tablets and represents a targeted therapy for certain non-small cell lung cancers and pancreatic cancer. The drug reversibly binds to the intracellular kinase domain of EGFR, blocking downstream signaling pathways critical for tumor cell proliferation and survival.

Mechanism of Action

Erlotinib inhibits the tyrosine kinase activity of EGFR (HER1/ErbB-1) by competing with adenosine triphosphate (ATP) for binding to the intracellular catalytic domain. This prevents autophosphorylation of tyrosine residues and blocks activation of downstream signaling cascades, including the Ras/Raf/MAPK and PI3K/Akt pathways. Inhibition of these pathways leads to cell cycle arrest, reduced angiogenesis, and induction of apoptosis in EGFR-dependent tumor cells.

Application

It is indicated for the first-line treatment of metastatic non-small cell lung cancer harboring EGFR exon 19 deletions or exon 21 (L858R) substitution mutations, as detected by an FDA-approved test. It is also indicated for maintenance therapy in patients with locally advanced or metastatic NSCLC following stabilization after first-line platinum-based chemotherapy. Additionally, it is approved in combination with gemcitabine for the first-line treatment of locally advanced, unresectable, or metastatic pancreatic cancer. Rash and diarrhea are the most common dose-limiting toxicities.

A systematic review of 10 trials (9 phase II, 1 phase III) evaluated erlotinib in advanced hepatocellular carcinoma. Tumor response rates varied widely: zero in four trials, below 10% in three, and above 20% in two. Disease control rates ranged from 42.5% to 79.6%. Most studies reported median progression‑free survival below 3.5 months, though three studies reported 6.5–9.0 months. Median overall survival ranged from 6.25 to 15.65 months. Grade 3/4 toxicities included fatigue (11.9%), diarrhea (10%), and rash (6.9%). The authors conclude erlotinib offers efficacy and tolerability, but better patient selection and well‑designed randomized trials are needed to improve outcomes.

Fig. 1 Study selection process for the systematic review of phase II/III trials of erlotinib for the treatment of unresectable or advanced hepatocellular carcinoma. (Zhang J, et al., 2016)

References

Zhang J, et al. Erlotinib for advanced hepatocellular carcinoma. A systematic review of phase II/III clinical trials. Saudi Med J. 2016; 37(11):1184-1190.

Using a systematic Quality‑by‑Design approach, erlotinib hydrochloride was encapsulated in chitosan‑PLGA nanoparticles. The optimized nanoparticles had a mean diameter of 226.5 nm, zeta potential of 27.7 mV, and entrapment efficiency of 78.9%. They exhibited homogeneous spherical morphology and sustained drug release over 72 hours. The systematic optimization of critical quality attributes provides a robust formulation strategy for improving the delivery of erlotinib in non‑small cell lung cancer.

Fig. 2 Characterization of ERT-HCL-Loaded CS-PLGA nanoparticles. (Nijhawan HP, et al., 2024)

References

Nijhawan HP, et al. Central composite design augmented quality-by-design-based systematic formulation of erlotinib hydrochloride-loaded chitosan-poly (lactic-co-glycolic acid) nanoparticles. Ther Deliv. 2024; 15(6):427-447.

Does Erlotinib Hydrochloride require refrigerated storage as a tyrosine kinase inhibitor?

No, it is stable at controlled room temperature (15-25°C). Refrigeration is not required, but avoid temperatures above 30°C to prevent potential degradation.

Is Erlotinib Hydrochloride sensitive to light and moisture?

Yes, it is both photosensitive and hygroscopic. Store in original, tightly sealed, light-resistant containers with desiccant to maintain chemical integrity.

What is the stability of Erlotinib Hydrochloride in tablet formulations?

It shows good stability when formulated with standard excipients and packaged in moisture-protective blisters.

How is the genotoxic impurity N-(3-ethynylphenyl)benzamide controlled?

We use a highly sensitive LC-MS/MS method to monitor this potential impurity, ensuring levels are below the threshold of toxicological concern (TTC).