Trametinib Dimethyl Sulfoxide is the pharmaceutical DMSO-solvate form of trametinib and a selective MEK1/MEK2 inhibitor used as an antineoplastic active pharmaceutical ingredient. It is a 1:1 stoichiometric DMSO solvate in which one molecule of trametinib is associated with one molecule of dimethyl sulfoxide in the crystal lattice. FDA identifies the substance by CAS 1187431-43-1, while the non-solvated trametinib parent has CAS 871700-17-3.
The molecular formula of Trametinib Dimethyl Sulfoxide is C₂₈H₂₉FIN₅O₅S, with a molecular weight of 693.53 g/mol. FDA and EMA describe it as a white to almost-white powder/solid.
Trametinib is a reversible, highly selective allosteric inhibitor of MEK1 and MEK2 activation and kinase activity. It acts on the MAPK/ERK signaling pathway, which is frequently activated in cancers carrying BRAF mutations.
Trametinib Dimethyl Sulfoxide is the active pharmaceutical substance used in MEKINIST. FDA documentation confirms that the DMSO-solvated form is used to provide the trametinib active moiety in the finished pharmaceutical product. For example, a 2 mg MEKINIST tablet contains 2.254 mg of Trametinib Dimethyl Sulfoxide, equivalent to 2 mg of non-solvated trametinib.
EMA confirms that the DMSO is fully incorporated into the crystal lattice. The commercial solid form is Form I, and the substance does not exhibit stereoisomerism. EMA also reports very low aqueous solubility across the physiological pH range.
| Property | Details |
|---|---|
| Product Name | Trametinib Dimethyl Sulfoxide |
| Active Moiety | Trametinib |
| CAS Number | 1187431-43-1 |
| Parent Trametinib CAS | 871700-17-3 |
| UNII | BSB9VJ5TUT |
| Development Code | GSK1120212B / GSK-1120212 |
| Molecular Formula | C₂₈H₂₉FIN₅O₅S |
| Alternative Formula Representation | C₂₆H₂₃FIN₅O₄·C₂H₆OS |
| Molecular Weight | 693.53 g/mol |
| API Type | Synthetic small-molecule API |
| Pharmacological Class | MEK1/MEK2 inhibitor |
| Therapeutic Class | Antineoplastic agent |
| ATC Code | L01EE01 |
| Physical Form | White to almost-white solid/powder |
| Solvate | 1:1 DMSO solvate |
| Stereochemistry | Achiral; no defined stereocenters |
| Aqueous Solubility | Very low / practically insoluble |
| Commercial Product | MEKINIST |
FDA GSRS identifies Trametinib Dimethyl Sulfoxide as the preferred substance name with UNII BSB9VJ5TUT and CAS 1187431-43-1.
Trametinib Dimethyl Sulfoxide is used as a targeted oncology API. Trametinib inhibits MEK1 and MEK2, components of the RAS/RAF/MEK/ERK pathway. This mechanism is particularly relevant to tumors driven by abnormal MAPK pathway signaling.
The finished MEKINIST product is used in approved oncology indications, including BRAF V600 mutation-positive melanoma and other BRAF V600-driven malignancies according to applicable regulatory labeling.
Swapnroop Drugs & Pharmaceuticals provides pharmaceutical API sourcing and supply support for Trametinib Dimethyl Sulfoxide for qualified pharmaceutical manufacturing, formulation-development and bulk API requirements.
As a Trametinib Dimethyl Sulfoxide API manufacturer and supplier in India, Swapnroop focuses on correct API-form identification, specification-based quality assessment, technical documentation, traceability and suitable pharmaceutical packaging.
Customers requiring Trametinib Dimethyl Sulfoxide can request product specifications, Certificate of Analysis, technical documentation and bulk supply information according to their requirements.
Trametinib Dimethyl Sulfoxide should be handled in accordance with the applicable drug-substance specification and validated stability conditions. EMA reports that the DMSO-solvated Form I is the controlled commercial solid form and that the solvate can desolvate under certain solvent, temperature and humidity conditions.
Appropriate protection from moisture, excessive heat and unsuitable environmental exposure should therefore be maintained.
Typical documentation may include:
Swapnroop Drugs & Pharmaceuticals supports pharmaceutical companies seeking Trametinib Dimethyl Sulfoxide API manufacturer and supplier services in India.
The supply approach emphasizes:
For bulk Trametinib Dimethyl Sulfoxide API requirements, customers can contact Swapnroop for availability, specifications, documentation and commercial supply information.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 99.0% – 101.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.1% |
| Heavy Metals | NMT 10 ppm |
| Individual Impurity | NMT 0.10% |
| Total Impurities | NMT 0.50% |
| Water Content | NMT 1.0% |