Milciclib
| Milciclib | |
|---|---|
| [[File:|frameless|220px|alt=|Chemical structure of Milciclib]] | |
| INN | |
| Drug class | |
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| CAS Number | 923032-37-5 |
| PubChem | 16047624 |
| DrugBank | |
| ChemSpider | 13196400 |
| KEGG | |
Milciclib is a small molecule inhibitor that targets multiple cyclin-dependent kinases (CDKs) and is being investigated for its potential use in cancer therapy. It is known by its research code PHA-848125.
Mechanism of Action
Milciclib functions primarily as a cyclin-dependent kinase inhibitor. CDKs are a family of protein kinases that play crucial roles in regulating the cell cycle. By inhibiting these kinases, Milciclib can interfere with the proliferation of cancer cells, potentially leading to cell cycle arrest and apoptosis.
Milciclib has been shown to inhibit CDK2, CDK5, and CDK7, among others. This broad spectrum of activity allows it to target various pathways involved in cancer cell growth and survival.
Clinical Development
Milciclib is currently undergoing clinical trials to evaluate its efficacy and safety in treating different types of cancer. It has shown promise in preclinical studies and early-phase clinical trials, particularly in hepatocellular carcinoma and thymic carcinoma.
Hepatocellular Carcinoma
In patients with hepatocellular carcinoma, Milciclib has been studied as a monotherapy and in combination with other agents. The drug has demonstrated the ability to stabilize disease progression and, in some cases, reduce tumor size.
Thymic Carcinoma
Milciclib has also been investigated for its effects on thymic carcinoma, a rare type of cancer. Preliminary results suggest that it may offer a therapeutic benefit for patients with this condition, particularly those who have not responded to conventional therapies.
Pharmacokinetics
Milciclib is administered orally, and its pharmacokinetic profile includes rapid absorption and a moderate half-life, allowing for convenient dosing schedules. The drug is metabolized primarily in the liver and excreted through the kidneys.
Side Effects
As with many cancer therapies, Milciclib can cause side effects. Common adverse effects include fatigue, nausea, and hematological abnormalities such as neutropenia and thrombocytopenia. Monitoring of blood counts and liver function is recommended during treatment.
Research and Future Directions
Ongoing research is focused on optimizing the use of Milciclib in combination with other therapeutic agents to enhance its efficacy and reduce resistance. Studies are also exploring its potential role in other malignancies beyond liver and thymic cancers.
Also see
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Contributors: Prab R. Tumpati, MD