Acalabrutinib

Acalabrutinib (trade name Calquence) is a medication used to treat a type of non-Hodgkin lymphoma known as mantle cell lymphoma. Specifically it is for people who had previously been treated with another therapy. It is unclear if it results in improved outcomes as of 2019. Acalabrutinib (trade name Calquence) is a medication used to treat a type of non-Hodgkin lymphoma known as mantle cell lymphoma. Specifically it is for people who had previously been treated with another therapy. It is unclear if it results in improved outcomes as of 2019. Common side effects include headaches, feeling tired, low red blood cells, low platelets, and low white blood cells. It is a second generation Bruton's tyrosine kinase inhibitor. Acalabrutinib was approved for medical use in the United States in 2017. The whole sale cost as of 2018 in the United States is 14,064 USD per month. It is used to treat a type of non-Hodgkin lymphoma known as mantle cell lymphoma. It is unclear if it results in improved outcomes as of 2019. The most common adverse events were headache, diarrhea and weight gain. Despite the appearance of a greater occurrence of transient headaches, data suggests a preferred advantage of acalabrutinib over ibrutinib due to expected reduced adverse events of skin rash, severe diarrhea, and bleeding risk. Acalabrutinib is the INN. As of February 2016, acalabrutinib had received orphan designation in the United States for CLL only, and was similarly designated as an orphan medicinal product by the European Medicines Agency (EMA) Committee for Orphan Medicinal Products (COMP) for treatment of three indications - chronic lymphocytic leukemia (CLL)/ small lymphocytic lymphoma (SLL), mantle cell lymphoma (MCL), and lymphoplasmacytic lymphoma (Waldenström's macroglobulinaemia, WM). If the drug is ultimately approved, this designation will result in a 10-year period of market exclusivity for the stated indications within Europe. It was developed by developed by Acerta Pharma. After the promising results for the treatment of CLL in initial clinical trials, Astra Zeneca purchased a 55% stake in Acerta Pharma for $4 billion in December 2015, with an option to acquire the remaining 45% stake for an additional $3 billion, conditional on the first approval in both the US and Europe and the establishment of commercial opportunity. Relative to ibrutinib, acalabrutinib demonstrated higher selectivity and inhibition of the targeted activity of BTK, while having a much greater IC50 or otherwise virtually no inhibition on the kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1. In addition, in platelets treated with ibrutinib, thrombus formation was clearly inhibited while no impact to thrombus formation was identified relative to controls for those treated with acalabrutinib. These findings strongly suggest an improved safety profile of acalabrutinib with minimized adverse effects relative to ibrutinib. In pre-clinical studies, it was shown to be more potent and selective than ibrutinib, the first-in-class BTK inhibitor.