Drug intelligence / Profile preview

erlotinib + gefitinib + icotinib + pamidronate + zoledronic acid

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of five drugs: three first-generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs)—erlotinib, gefitinib, and icotinib—and two bisphosphonates—pamidronate and zoledronic acid. Erlotinib, gefitinib, and icotinib are small molecule inhibitors that selectively block the tyrosine kinase activity of the EGFR, thereby inhibiting downstream signaling pathways involved in cell proliferation and survival. These agents are primarily used for the treatment of non-small cell lung cancer (NSCLC) with activating EGFR mutations[1][2][3][4]. Pamidronate and zoledronic acid are nitrogen-containing bisphosphonates that inhibit osteoclast-mediated bone resorption by binding to hydroxyapatite in bone tissue. They are used to prevent skeletal-related events in patients with bone metastases from cancers such as breast cancer or multiple myeloma[7][9]. Zoledronic acid is considered more potent than pamidronate for these indications[7][9].

Brand names
Tarceva (erlotinib)Iressa (gefitinib)Conmana (icotinib)Aredia (pamidronate)Zometa (zoledronic acid)
02

Targets

FDPS (Farnesyl pyrophosphate synthase)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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