Inavolisib is a small-molecule phosphatidylinositol 3-kinase alpha (PI3Kα) inhibitor and active pharmaceutical ingredient used in oncology. It is a selective and potent inhibitor of the PI3Kα pathway, including mutant forms of the PIK3CA gene that can contribute to tumor growth.
Inavolisib has the molecular formula C24H27F2N5O3 and a molecular weight of approximately 471.51 g/mol. Its CAS Number is 2060571-02-8.
Inavolisib is an orally active targeted anticancer compound developed for cancers characterized by specific PIK3CA mutations. By selectively inhibiting PI3Kα signaling, inavolisib can interfere with downstream pathways involved in tumor-cell proliferation, survival and metabolism.
It is particularly associated with the treatment of PIK3CA-mutated, hormone receptor-positive, HER2-negative locally advanced or metastatic breast cancer in combination with other anticancer agents, according to approved indications.
Inavolisib selectively inhibits the PI3Kα catalytic subunit, encoded by the PIK3CA gene.
Inhibition of PI3Kα reduces downstream AKT/mTOR signaling, which can suppress growth and survival signals in tumor cells carrying activating PIK3CA mutations. Inavolisib also has properties that promote degradation of mutant p110α protein, contributing to sustained pathway inhibition.
Inavolisib API is used in the development and manufacture of:
Inavolisib is manufactured through controlled chemical synthesis followed by purification, crystallization and drying. Quality control evaluates chemical identity, assay, related substances and other critical quality attributes.
Testing may include HPLC/UPLC purity, identification by spectroscopic techniques, residual solvents, water content, elemental impurities and other parameters according to the applicable approved specification.
Inavolisib is generally supplied as a white to off-white solid/crystalline powder. It has limited aqueous solubility and is handled as a pharmaceutical-grade small-molecule API.
Inavolisib should be stored in a tightly closed container under controlled conditions and protected from excessive moisture, heat and direct light. Storage requirements should follow the manufacturer's current CoA, SDS and validated stability data.
Depending on the intended pharmaceutical application, documentation may include:
Inavolisib is a targeted PI3Kα inhibitor designed to address cancers driven by activating PIK3CA mutations. Its selective pathway inhibition makes it an important pharmaceutical ingredient for precision oncology and targeted treatment development.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | Complies with applicable ICH Q3D limits |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 2.0% |