Introduction
Cabozantinib, developed by Exelis Inc. as initially XL185, was first FDA approved in 2012 under the brand name CometriqTM. There are two formulations of cabozantinib in which CometriqTM is an oral capsule and has the clinical advantage of a quicker delivery time in comparison to its tablet form (CabometyxTM). Bioequivalence for the formulations are not the same, a 19% higher Cmax for the tablet form, and should not be used interchangeably. The current essay will focus on the drug characteristics of cabozantinib, specifically its mechanism of action, pharmacokinetics (bioavailability, metabolism, distribution and excretion) and the pharmacodynamics as a result of the former, use in treatment and adverse effects found in clinical trials. A preliminary background on the development of cancer is first described to understand the targets and actions of cabozantinib, with a particular emphasis on medullary thyroid cancer.
The development of cancer
Cancer is one of the leading causes of illnesses in Australia. …show more content…
The Cmax (peak plasma concentration) of oral administration was at a median of 4 hours (Nguyen, et al., 2015). [Cabozantinib has a high protein affinity in human plasma (>99.7%). A high-fat meal moderately increased Cmax and AUC values relative to fasting conditions in healthy volunteers. Steady state achieved by approximately day 15. The long half-life was estimated at 91.3 33.4 hours (mean standard deviation) with a subjective comparison of an effective half-life at 55h for males and 70h in females (62.5h in combination) lower in the subsequent literature (Kuzrock, et al., 2011; Miles, et al., 2016). The approximate volume of distribution is about 349 L (Miles, et al., 2016). Repeated dosing may cause drug
Cabozantinib, developed by Exelis Inc. as initially XL185, was first FDA approved in 2012 under the brand name CometriqTM. There are two formulations of cabozantinib in which CometriqTM is an oral capsule and has the clinical advantage of a quicker delivery time in comparison to its tablet form (CabometyxTM). Bioequivalence for the formulations are not the same, a 19% higher Cmax for the tablet form, and should not be used interchangeably. The current essay will focus on the drug characteristics of cabozantinib, specifically its mechanism of action, pharmacokinetics (bioavailability, metabolism, distribution and excretion) and the pharmacodynamics as a result of the former, use in treatment and adverse effects found in clinical trials. A preliminary background on the development of cancer is first described to understand the targets and actions of cabozantinib, with a particular emphasis on medullary thyroid cancer.
The development of cancer
Cancer is one of the leading causes of illnesses in Australia. …show more content…
The Cmax (peak plasma concentration) of oral administration was at a median of 4 hours (Nguyen, et al., 2015). [Cabozantinib has a high protein affinity in human plasma (>99.7%). A high-fat meal moderately increased Cmax and AUC values relative to fasting conditions in healthy volunteers. Steady state achieved by approximately day 15. The long half-life was estimated at 91.3 33.4 hours (mean standard deviation) with a subjective comparison of an effective half-life at 55h for males and 70h in females (62.5h in combination) lower in the subsequent literature (Kuzrock, et al., 2011; Miles, et al., 2016). The approximate volume of distribution is about 349 L (Miles, et al., 2016). Repeated dosing may cause drug