Palbociclib specifically is an orally existing CDK inhibitor with antineoplastic activity. It has potential and selectively inhibits the CDK4 and CDK6, thereby inhibiting the Rb protein phosphorylation early in the G1 phase leading to the cell cycle arrest. This helps suppress the DNA replication as well as reduces the tumor cell proliferation. CDK4 and CDK6 are the serine/threonine kinases that are upregulated in the several tumor cell types and play a crucial role in order to regulate the cell cycle progression.
Palbociclib is a unique CDK inhibitor, used along with the aromatase inhibitors in order to treat postmenopausal women with metastatic breast cancer. Palbociclib is linked with transient and usually mild elevations in the serum aminotransferase during therapy and to an unusual form of liver injury named pseudocirrhosis caused due to shrinkage of tumor metastases in the liver combined with desmoplastic changes and vascular damage, that may be severe, progressive and fatal.
Approval: In the month of March, 2017, the U.S. FDA granted the regular approval to palbociclib tablet for the treatment of HR positive, HER2 negative advanced/metastatic breast cancer along with an aromatase inhibitor as an initial endocrine based therapy in the postmenopausal women.
In the month of February, 2015, FDA granted palbociclib accelerated approval together with letrozole for treating the estrogen receptor (ER)-positive, HER2-negative advanced breast cancer as an initial endocrine based therapy in postmenopausal women. The Food and Drug Administration granted palbociclib regular approval in the month of February 2016, along with fulvestrant for treating the HR+, HER2- advanced/metastatic breast cancer in women with disease progression after the endocrine therapy.
Dosage Form: Palbociclib comes in the form of capsules generically and under the brand name Ibrance. The recommended daily dose of palbociclib 125 mg capsule administered orally once in a day for 21 (3-week) consecutive days followed by the 7-days off treatment to comprise a full cycle of 28 days. Palbociclib should be administered through food. Administer the recommended dose of an aromatase inhibitor when given together with Palbociclib. When prescribed with palbociclib, the recommended fulvestrant dose is 500 mg should be administered on Days 1, 15, 29, and once monthly thereafter.
Respective patients should be encouraged to take their palbociclib dose at approximately the same time each day.
Side Effects: Side effects of palbociclib are usually mild and not life threatening. The commonly reported side effects may include fatigue, neutropenia, infections, leukopenia, nausea, stomatitis, vomiting, anemia, alopecia, diarrhea, thrombocytopenia, rash, decreased appetite, asthenia, and pyrexia.
Price: The palbociclib cost in India may vary depending on the wholesaler/pharmacy and of course the brand you choose. The cost of palbociclib is reasonable at every WHO-GDP & ISO certified wholesaler/pharmacy.
This information is earlier published here
