A Clinical Trial to Evaluate Pharmacokinetic Interactions and Safety Between Fimasartan and Linagliptin in Healthy Male Volunteers

This is an open-label, randomized, multiple-dose, two-period and single-sequence study to evaluate the pharmacokinetics and safety.

• (fimasartan or linagliptin) x 7days (Drug): Part A: fimasartan, Part B: linagliptin
• (fimasartan and linagliptin) x 7days (Drug): Part A \& Part B: Co-administration of fimasartan and linagliptin

Primary outcomes

• [Part A] AUC of fimasartan [0~24 hour after drug administration]: \[Part A\] Area under the curve(AUC) of fimasartan in steady state
• [Part A] Cmax of fimasartan [0~24 hour after drug administration]: \[Part A\] Cmax of fimasartan in steady state
• [Part B] AUC of Linagliptin [0~24 hour after drug administration]: \[Part B\] Area under the curve(AUC) of Linagliptin in Steady State
• [Part B] Cmax of linagliptin [0~24 hour after drug administration]: \[Part B\] Cmax of linagliptin in steady state

Sex: Male, ages: 19 Years to 50 Years, accepts healthy volunteers

1\. Inclusion Criteria (Total: 5):

1. 19-50 year-old healthy male.
2. 18.5kg/m2 ≤ Body mass index(BMI) ≤ 27kg/m2
3. Subject who has no clinically significant medical history.
4. Subject whose informed consent is obtained and who is willing to comply with protocol.

2\. Exclusion Criteria (Total: 19):

1. Sitting systolic blood pressure(SiSBP) ≥ 140mmHg or < 115mmHg / Sitting Diastolic blood pressure(SiDBP) ≥ 90mmHg or < 70mmHg
2. Upper Limits of Normal x 1.5 < Aspartate transaminase(AST), Alanine transminase(ALT), Total bilirubin
3. Creatinine clearance(CrCl) < 80mL/min (using Cockcroft-Gault formula)
4. Positive results in HBsAg, Hepatitis C virus(HCV) Ab, HIV Ag/Ab, Venereal disease research laboratory(VDRL)
5. Participate in another clinical trial within 12 weeks prior to the first administration of Investigational product(IP).

• Results publication: Kang WY, Lee HW, Gwon MR, Cho S, Shim WS, Lee KT, Yang DH, Seong SJ, Yoon YR. A Pharmacokinetic Drug Interaction Between Fimasartan and Linagliptin in Healthy Volunteers. Drug Des Devel Ther. 2020 May 26;14:2101-2111. doi: 10.2147/DDDT.S248205. eCollection 2020. PMID 32546973

• Young-Ran Yoon, PhD, Principal investigator, Kyungpook National University Hospital