Abemaciclib specifically is the third small molecule orally bioavailable inhibitor of CDK4 and CDK6. This agent is structurally different to ribociclib and palbociclib, in that it exhibits a greater selectivity for the CDK4 in vitro.
One group fortunately showed the ability of the abemaciclib in order to exert the CDK4/6 inhibition and subsequent cell arrest in the mice bearing human colorectal xenografts, as well as demonstrating ensuing tumour growth inhibition, later validating those findings in the human melanoma xenografts.
This study favoured the therapeutic dose as well as the continuous dosing way employed in the abemaciclib clinical studies, showing that the steady-state trough plasma concentrations were achieved by continuous dosing, which managed the durable cell-cycle arrest. Rodent xenograft studies by another group demonstrated abemaciclib can cross the blood brain barrier, with active levels reached quite efficiently, and at reduced doses, than with the palbociclib.
Approval: Designated as a breakthrough therapy in order to treat breast cancer by the U.S. Food and Drug Administration (FDA), Abemaciclib was approved on 28'th September in the year of 2017 for use in the United States.
Dosage Form: When used as a monotherapy, the recommended abemaciclib dose is 200mg, which should be taken orally twice a day. If it is taken as part of a combination therapy (i.e. alongside fulvestrant or hormone therapy) the standard recommended dose is abemaciclib 150 mg twice daily.
Dosage of abemaciclib may also be modified in order to reduce the adverse treatment effects. In case the patient cannot tolerate the initial dose of 200 mg, it will be reduced to 150 mg, then 100 mg, then 50 mg. In case the patient is unable to tolerate a 50 mg dose, treatment with abemaciclib will be stopped.
Side Effects: Side effects of abemaciclib 150 mg may range from mild to serious including diarrhea, vomiting, nausea, severe abdominal pain, decreased appetite, hair loss, headache, and fatigue.
Cost: The abemaciclib cost in India may vary depending on the wholesaler/pharmacy and of course the brand you choose. The cost of an abemaciclib is around INR for a supply of capsules.
Clinical Statistics: The efficacy of abemaciclib as a treatment for metastatic breast cancer has been demonstrated in a series of clinical trials named MONARCH-1, MONARCH-2 and MONARCH-3.
Findings from all the three trials found that the treatment with abemaciclib (when used along with hormone therapy) significantly resisted the progression of cancer and prolonged the overall survival in patients with breast cancer.
Abemaciclib was also demonstrated to significantly reduce the size of tumor, with an average reduction of 76.1% following 24 cycles of treatment noted in the MONARCH-3 study.
Treatment with abemaciclib was also found to significantly improve the PFS (Progression-free Survival) among patients with metastatic breast cancer.
Source url:- https://amit59.doodlekit.com/blog/entry/15211764/what-are-the-medical-uses-of-abemaciclib
