Tepotinib is an orally active, selective MET tyrosine kinase inhibitor (TKI) used in oncology. The pharmaceutical product TEPMETKO contains tepotinib hydrochloride hydrate, while the active moiety is tepotinib. Tepotinib selectively inhibits MET signaling, including signaling associated with MET exon 14 skipping alterations, which can drive tumor-cell proliferation, survival, migration and invasion.
The free-form tepotinib has the molecular formula C29H28N6O2 and molecular weight 492.58 g/mol. Its pharmaceutical form, tepotinib hydrochloride hydrate, has the formula C29H28N6O2·HCl·H2O and molecular weight 547.05 g/mol. The FDA label identifies the hydrochloride hydrate as the material used in TEPMETKO.
For your product page, I recommend using Tepotinib Hydrochloride Hydrate in the Product Data section rather than treating 492.58 g/mol as the molecular weight of the marketed API form.
| Parameter | Value |
|---|---|
| Product Name | Tepotinib |
| Pharmaceutical Form | Tepotinib Hydrochloride Hydrate |
| CAS No. | 1946826-82-9 |
| Free-Base CAS | 1100598-32-0 |
| FDA UNII | VY5YX2TQ1F |
| Development Code | MSC2156119 / EMD-1214063 |
| Molecular Formula – Free Base | C29H28N6O2 |
| Molecular Weight – Free Base | 492.58 g/mol |
| Molecular Formula – HCl Hydrate | C29H28N6O2·HCl·H2O |
| Molecular Weight – HCl Hydrate | 547.05 g/mol |
| Therapeutic Class | Antineoplastic |
| Drug Class | MET Tyrosine Kinase Inhibitor |
| Target | MET / c-MET |
| Physical Form | White to off-white powder |
FDA and DailyMed identify tepotinib hydrochloride hydrate as the pharmaceutical drug substance used in TEPMETKO.
PubChem identifies CAS 1946826-82-9 for the hydrochloride hydrate and CAS 1100598-32-0 for the anhydrous hydrochloride/free-form records.
Tepotinib is a small-molecule kinase inhibitor designed to selectively inhibit the mesenchymal-epithelial transition factor (MET) receptor tyrosine kinase.
The free base has a molecular weight of 492.58 g/mol, while the pharmaceutical hydrochloride hydrate has a molecular weight of 547.05 g/mol. The difference is important when calculating assay basis, formulation equivalence and API quantity.
Tepotinib hydrochloride hydrate is described as a white to off-white powder and has a reported pKa of 9.5. It is a low-solubility compound with strongly pH-dependent solubility.
The pharmaceutical substance is non-hygroscopic according to the product information reviewed by EMA and other regulatory documentation.
Tepotinib selectively targets the MET receptor tyrosine kinase.
MET can be activated by hepatocyte growth factor (HGF), leading to downstream signaling pathways that regulate cell proliferation, survival, migration and invasion. Tepotinib inhibits both HGF-dependent and HGF-independent MET phosphorylation and suppresses MET-dependent downstream signaling.
This mechanism is particularly relevant to tumors carrying MET exon 14 skipping alterations, in which abnormal MET signaling can promote oncogenic activity.
Tepotinib API is used in the manufacture of oncology medicines intended for MET-driven cancers.
Its principal pharmaceutical application is:
The FDA-approved TEPMETKO indication is for adults with metastatic NSCLC whose tumors have MET exon 14 skipping alterations.
Tepotinib hydrochloride hydrate is a chemically synthesized small-molecule API and should be characterized using a comprehensive pharmaceutical analytical package.
Appropriate controls can include:
The exact numerical acceptance criteria should come from the applicable approved drug-substance specification. I could not verify a public universal BP/Ph. Eur./USP monograph containing the complete numerical release limits for tepotinib hydrochloride hydrate, so those fields should not be populated with invented numbers.
Tepotinib is a synthetic small-molecule pharmaceutical API. Manufacturing involves controlled chemical synthesis, purification and isolation of the required pharmaceutical form.
For a commercial API manufacturing process, important quality attributes include:
Because the approved pharmaceutical substance is specifically tepotinib hydrochloride hydrate, control of hydration state and solid form is particularly important.
The pKa and pharmaceutical-form data are supported by FDA labeling and product information; the calculated XLogP3-AA and TPSA are from PubChem.
Tepotinib has pH-dependent aqueous solubility.
Regulatory documentation describes tepotinib as:
Therefore, I recommend entering “pH-dependent solubility” in the CMS Solubility field rather than using an unsupported single mg/mL number.
Tepotinib API should be stored in an appropriate pharmaceutical-grade container that protects the material from contamination and environmental exposure.
The finished TEPMETKO product is stored at 20–25°C, with permitted excursions between 15–30°C. This is a finished-product storage condition and should not automatically be treated as the API storage specification.
For bulk API, the manufacturer's validated stability program should determine the:
A pharmaceutical Tepotinib API manufacturer should maintain appropriate documentation including:
Tepotinib is a specialized oncology API requiring control of chemical purity, related substances, solid-state characteristics and the correct hydrochloride hydrate form.
A qualified Tepotinib API manufacturer in India should maintain validated analytical methods, controlled chemical synthesis, appropriate impurity controls and consistent batch quality.
For pharmaceutical customers, it is particularly important to confirm whether the required material is tepotinib free base, tepotinib hydrochloride anhydrous or tepotinib hydrochloride hydrate, because these forms have different molecular formulas and molecular weights.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |