Description

Erlotinib hydrochloride is an Organic compound with the chemical formula C22H24ClN3O4. It is soluble in DMSO even up to 18 mg/ml with warming. Erlotinib hydrochloride is a member of a class of targeted anticancer drugs that inhibit the activity of the epidermal growth factor receptor. It is sold under the brand names Tarceva, OSI Pharmaceuticals, Genentech, and Roche among others.

Polymorphism in Erlotinib Hydrochloride

The polymorphism of Erlotinib hydrochloride is still ill-characterized. But as a lipophilic anticancer drug, it is an essential component of the current armamentarium for the treatment of pancreatic and lung cancers[1]. The two most important EtbHCl polymorphs are forms A and B. Studies have found that form B is more stable than form A at, or close to, ambient temperature and that the larger stability of form B is enthalpically determined (hence of lattice energy origin). In addition, the solubility measurements (gastric fluid at pH 1.2, 298 ± 1 K) evidenced a 2.6 times larger solubility of form A relative to form B. Consequently, a significant bioavailability enhancement may be potentially obtained if form A rather than form B is used in EtbHCl formulations[2].

Uses

As an effective anti-cancer drug, it is currently being used to treat Lung cancer and Pancreatic cancer. This drug was approved by the US FDA in November 2004 for the treatment of advanced non-small-cell lung cancer after failure of at least one prior chemotherapy regimen. In November 2005, the FDA approved erlotinib in combination with gemcitabine for the treatment of locally advanced, unresectable, or metastatic pancreatic cancer. But side effects such as Rash, Diarrhea, Loss of appetite, Fatigue, and Partial hair loss need attention[3].

References

[1] Catarina T, et al. Polymorphism in Erlotinib Hydrochloride: New Insights into Relative Stability, Thermal Behavior, and Structural Differences of Forms A and B. Crystal Growth & Design, 2023. 

[2] Soni G, et al. QbD based approach for formulation development of spray dried microparticles of erlotinib hydrochloride for sustained release. Journal of Drug Delivery Science and Technology, 2020; 57: 101684. 

[3] Minna, et al. Erlotinib hydrochloride. Nature Reviews Drug Discovery , 2005.