Lomustine is an orally active alkylating antineoplastic agent belonging to the nitrosourea class. It is a lipophilic chemotherapy drug that can cross the blood-brain barrier, making it particularly relevant in the treatment of certain brain tumors and other cancers.
Lomustine acts by producing reactive alkylating species that damage DNA and interfere with DNA replication and cellular proliferation. It is also known by the development code CCNU.
Lomustine is a specialized oncology pharmaceutical API used in the manufacture of oral anticancer formulations. Its production requires controlled synthesis, purification and stringent quality-control testing because nitrosourea compounds require careful handling and characterization.
Important quality attributes include identity, assay, related substances, water content, residue on ignition and residual solvents.
CAS Number: 13010-47-4
Molecular Formula: C9H16ClN3O2
Molecular Weight: 233.69 g/mol
Synonym: CCNU
Chemical Name: 1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea
Drug Class: Nitrosourea Alkylating Agent
Therapeutic Class: Antineoplastic Agent
Therapeutic Area: Oncology
Molecule Type: Synthetic Small Molecule
Lomustine undergoes decomposition to form reactive metabolites capable of alkylating DNA and other cellular macromolecules.
DNA damage caused by these reactive intermediates interferes with:
Its lipophilic nature allows Lomustine to cross the blood-brain barrier, contributing to its use in certain central nervous system malignancies.
Lomustine is used in oncology treatment regimens for certain:
Its clinical use depends on the approved indication, treatment protocol and applicable regulatory labeling.
Lomustine is particularly relevant to central nervous system oncology because of its ability to penetrate the blood-brain barrier.
It may be used alone or as part of combination chemotherapy regimens depending on the cancer type and treatment protocol.
Lomustine is generally described as a yellow crystalline powder. It is practically insoluble in water and has greater solubility in certain organic solvents.
A controlled Lomustine API manufacturing process may involve:
Because Lomustine is a nitrosourea compound, manufacturing controls should include appropriate containment, impurity control and validated analytical procedures.
Typical Lomustine API testing may include:
Store Lomustine API in a tightly closed container under controlled pharmaceutical storage conditions, protected from heat, moisture and direct light. The final storage requirements should follow validated stability data and the applicable approved API specification.
Lomustine is relevant to research involving:
Lomustine is a nitrosourea alkylating anticancer API with CAS Number 13010-47-4, molecular formula C9H16ClN3O2, and molecular weight 233.69 g/mol. Also known as CCNU, it produces DNA damage through alkylation and is notable for its ability to cross the blood-brain barrier.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | Conforms by IR and HPLC |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 1.0% |
| Melting Point | Approximately 90°C – 95°C |