Evaluation of the pharmacokinetics and food effects of a novel formulation tamsulosin 0.4 mg capsule compared with a 0.2 mg capsule in healthy male volunteers

Tamsulosin, an alpha-1 adrenoreceptor antagonist, has been used as a primary option for medical treatment of benign prostate hyperplasia. An open-label, single-dose, randomized, three-treatment, three-period, three sequence crossover study was conducted to evaluate the pharmacokinetics (PKs) of 0.2 and 0.4 mg tamsulosin hydrochloride (HCl) in the fed versus the fasted state. Subjects were randomly assigned to three sequences and received one of the following treatments at each period: tamsulosin HCl 0.2 or 0.4 mg in the fed state with a high-fat meal, or tamsulosin HCl 0.4 mg in the fasted state. Blood samples for the PK analysis were collected at pre-dose and up to 48 h post-dose. The PK parameters were calculated by a non-compartmental method. The geometric mean ratio (GMR) and its 90% confidence intervals (CIs) of the plasma maximum concentration (C max ) and area under concentration curve from time zero to last measurable concentration (AUClast) were calculated. Twenty-two subjects completed the study. The systemic exposure of tamsulosin 0.4 mg decreased approximately 9% in the fed state compared to the fasted state, and the time to reach peak concentration was slightly delayed in the fed state. The dose normalized GMR and its 90% CIs of C max and AUClast for 0.2 and 0.4 mg tamsulosin in the fed state were within 0.8 and 1.25 range. Systemic exposure of tamsulosin was decreased in the fed condition compared to the fasted condition. Linear PK profiles were observed between 0.2 and 0.4 mg tamsulosin in the fed state.

Pharmacogenomic information from CPIC and DPWG guidelines and its application on drug labels

There are several hurdles to overcome before implementing pharmacogenomics (PGx) in precision medicine. One of the hurdles is unawareness of PGx by clinicians due to insufficient pharmacogenomic information on drug labels. Therefore, it might be important to implement PGx that reflects pharmacogenomic information on drug labels, standard of prescription for clinicians. This study aimed to evaluate the level at which PGx was being used in clinical practice by comparing the Clinical Pharmacogenetics Implementation Consortium and Dutch Pharmacogenetics Working Group guidelines and drug labels of the US Food and Drug Administration (FDA) and the Korea Ministry of Food and Drug Safety (MFDS). Two PGx guidelines and drugs labels were scrutinized, and the concordance of the pharmacogenomic information between guidelines and drug labels was confirmed. The concordance of the label between FDA and MFDS was analyzed. In FDA labels, the number of concordant drug with guidelines was 24, while 13 drugs were concordant with MFDS labels. The number of drugs categorized as contraindication, change dose, and biomarker testing required was 7, 12 and 12 for the FDA and 8, 5 and 4 for the MFDS, respectively. The pharmacogenomic information of 9 drugs approved by both FDA and MFDS was identical. In conclusion, pharmacogenomic information on clinical implementation guidelines was limited on both FDA and MFDS labels because of various reasons including the characteristics of the guidelines and the drug labels. Therefore, more effort from pharmaceutical companies, academia and regulatory affairs needs to be made to implement pharmacogenomic information on drug labels.

Evaluation of the pharmacokinetics and food effects of a novel formulation tamsulosin 0.4 mg capsule compared with a 0.2 mg capsule in healthy male volunteers

Tamsulosin, an alpha-1 adrenoreceptor antagonist, has been used as a primary option for medical treatment of benign prostate hyperplasia. An open-label, single-dose, randomized, three-treatment, three-period, three sequence crossover study was conducted to evaluate the pharmacokinetics (PKs) of 0.2 and 0.4 mg tamsulosin hydrochloride (HCl) in the fed versus the fasted state. Subjects were randomly assigned to three sequences and received one of the following treatments at each period: tamsulosin HCl 0.2 or 0.4 mg in the fed state with a high-fat meal, or tamsulosin HCl 0.4 mg in the fasted state. Blood samples for the PK analysis were collected at pre-dose and up to 48 h post-dose. The PK parameters were calculated by a non-compartmental method. The geometric mean ratio (GMR) and its 90% confidence intervals (CIs) of the plasma maximum concentration (C max ) and area under concentration curve from time zero to last measurable concentration (AUClast) were calculated. Twenty-two subjects completed the study. The systemic exposure of tamsulosin 0.4 mg decreased approximately 9% in the fed state compared to the fasted state, and the time to reach peak concentration was slightly delayed in the fed state. The dose normalized GMR and its 90% CIs of C max and AUClast for 0.2 and 0.4 mg tamsulosin in the fed state were within 0.8 and 1.25 range. Systemic exposure of tamsulosin was decreased in the fed condition compared to the fasted condition. Linear PK profiles were observed between 0.2 and 0.4 mg tamsulosin in the fed state.

Pharmacogenomic information from CPIC and DPWG guidelines and its application on drug labels

There are several hurdles to overcome before implementing pharmacogenomics (PGx) in precision medicine. One of the hurdles is unawareness of PGx by clinicians due to insufficient pharmacogenomic information on drug labels. Therefore, it might be important to implement PGx that reflects pharmacogenomic information on drug labels, standard of prescription for clinicians. This study aimed to evaluate the level at which PGx was being used in clinical practice by comparing the Clinical Pharmacogenetics Implementation Consortium and Dutch Pharmacogenetics Working Group guidelines and drug labels of the US Food and Drug Administration (FDA) and the Korea Ministry of Food and Drug Safety (MFDS). Two PGx guidelines and drugs labels were scrutinized, and the concordance of the pharmacogenomic information between guidelines and drug labels was confirmed. The concordance of the label between FDA and MFDS was analyzed. In FDA labels, the number of concordant drug with guidelines was 24, while 13 drugs were concordant with MFDS labels. The number of drugs categorized as contraindication, change dose, and biomarker testing required was 7, 12 and 12 for the FDA and 8, 5 and 4 for the MFDS, respectively. The pharmacogenomic information of 9 drugs approved by both FDA and MFDS was identical. In conclusion, pharmacogenomic information on clinical implementation guidelines was limited on both FDA and MFDS labels because of various reasons including the characteristics of the guidelines and the drug labels. Therefore, more effort from pharmaceutical companies, academia and regulatory affairs needs to be made to implement pharmacogenomic information on drug labels.