Mobocertinib is an orally active small-molecule EGFR tyrosine kinase inhibitor (TKI) developed specifically to target EGFR exon 20 insertion mutations. It was developed under the codes TAK-788 and AP32788 and was marketed in the United States as Exkivity (mobocertinib).
Mobocertinib works by binding irreversibly to mutant EGFR and inhibiting receptor-mediated signaling involved in cancer-cell proliferation and survival. Its development focused particularly on non-small cell lung cancer (NSCLC) associated with EGFR exon 20 insertion mutations.
Important regulatory note: The FDA's accelerated approval for Exkivity was subsequently withdrawn on July 15, 2024. Therefore, current website content should describe Mobocertinib as a previously approved/investigational oncology compound rather than implying that its former U.S. indication remains FDA-approved.
PubChem and FDA GSRS identify Mobocertinib with CAS 1847461-43-1, formula C₃₂H₃₉N₇O₄, and molecular weight 585.7 g/mol.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | ≤ 0.5% |
| Total Impurities | ≤ 1.5% |