Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 52, 2022 - Issue 6
1,006
Views
0
CrossRef citations to date
0
Altmetric
Animal Pharmacokinetics and Metabolism

Selection of the candidate compound at an early stage of new drug development: retrospective pharmacokinetic and metabolic evaluations of valsartan using common marmosets

ORCID Icon, ORCID Icon, ORCID Icon, ORCID Icon, , , , , ORCID Icon & show all
Pages 613-624 | Received 01 Aug 2022, Accepted 18 Sep 2022, Published online: 05 Oct 2022

References

  • Anand IS, Deswal A, Kereiakes DJ, Purkayastha D, Zappe DH. 2010. Comparison of once-daily versus twice-daily dosing of valsartan in patients with chronic stable heart failure. Vasc Health Risk Manag. 6:449–455.
  • Bottorff MB, Tenero DM. 1999. Pharmacokinetics of eprosartan in healthy subjects, patients with hypertension, and special populations. Pharmacotherapy. 19(4 Pt 2):73S–78S.
  • Criscione L, Bradley WA, Bühlmayer P, Whitebread S, Glazer R, Lloyd P, Mueller P, Gasparo M. 1995. Valsartan: preclinical and clinical profile of an antihypertensive angiotensin-II antagonist. Cardiovasc Drug Rev. 13(3):230–250.
  • Di L, Feng B, Goosen TC, Lai Y, Steyn SJ, Varma MV, Obach RS. 2013. A perspective on the prediction of drug pharmacokinetics and disposition in drug research and development. Drug Metab Dispos. 41(12):1975–1993.
  • European Medicines Agency. 2009. ICH topic M3 (R2) non-clinical safety studies for the conduct of human clinical trials and marketing authorization for pharmaceuticals. London (UK): European Medicines Agency.
  • Flesch G, Müller P, Lloyd P. 1997. Absolute bioavailability and pharmacokinetics of valsartan, an angiotensin II receptor antagonist, in man. Eur J Clin Pharmacol. 52(2):115–120.
  • Food and Drug Administration. 1996. Drug Approval Package: Diovan (Valsartan) NDA#020665, Review and evaluation of pharmacology and toxicology data. https://www.accessdata.fda.gov/drugsatfda_docs/nda/pre96/020665_s000.pdf. (CDER’s historical data file)
  • Food and Drug Administration. 2016. Guidance for industry: safety testing of drug metabolites. Silver Spring (MD): US Department Health and Human Services FaDA, Center for Drug Evaluation and Research.
  • Göktaş MT, Pepedil F, Karaca Ö, Kalkışım S, Cevik L, Gumus E, Guven GS, Babaoglu MO, Bozkurt A, Yasar U. 2016. Relationship between genetic polymorphisms of drug efflux transporter MDR1 (ABCB1) and response to losartan in hypertension patients. Eur Rev Med Pharmacol Sci. 20(11):2460–2467.
  • Hamid KA, Lin Y, Gao Y, Katsumi H, Sakane T, Yamamoto A. 2009. The effect of Wellsolve, a novel solubilizing agent, on the intestinal barrier function and intestinal absorption of griseofulvin in rats. Biol Pharm Bull. 32(11):1898–1905.
  • Hedner T, Himmelmann A. 1999. The efficacy and tolerance of one or two daily doses of eprosartan in essential hypertension. J Hypertens. 17(1):129–136.
  • Hirvensalo P, Tornio A, Launiainen T, Paile‐Hyvärinen M, Tapaninen T, Neuvonen M, Backman JT, Niemi M. 2020. UGT1A3 and sex are major determinants of telmisartan pharmacokinetics-a comprehensive pharmacogenomic study. Clin Pharmacol Ther. 108(4):885–895.
  • Holwerda NJ, Fogari R, Angeli P, Porcellati C, Hereng C, Oddou-Stock P, Heath R, Bodin F. 1996. Valsartan, a new angiotensin II antagonist for the treatment of essential hypertension: efficacy and safety compared with placebo and enalapril. J Hypertens. 14(9):1147–1151.
  • Hosea NA, Collard WT, Cole S, Maurer TS, Fang RX, Jones H, Kakar SM, Nakai Y, Smith BJ, Webster R, et al. 2009. Prediction of human pharmacokinetics from preclinical information: comparative accuracy of quantitative prediction approaches. J Clin Pharmacol. 49(5):513–533.
  • Hughes JP, Rees S, Kalindjian SB, Philpott KL. 2011. Principles of early drug discovery. Br J Pharmacol. 162(6):1239–1249.
  • Huskey SE, Miller RR, Chiu SH. 1993. N-glucuronidation reactions. I. Tetrazole N-glucuronidation of selected angiotensin II receptor antagonists in hepatic microsomes from rats, dogs, monkeys, and humans. Drug Metab Dispos. 21(5):792–799.
  • Iriarte G, Ferreirós N, Ibarrondo I, Alonso RM, Maguregui MI, Jiménez RM. 2007. Biovalidation of an SPE-HPLC-UV-fluorescence method for the determination of valsartan and its metabolite valeryl-4-hydroxy-valsartan in human plasma. J Sep Sci. 30(14):2231–2240.
  • Jones RD, Jones HM, Rowland M, Gibson CR, Yates JWT, Chien JY, Ring BJ, Adkison KK, Ku MS, He H, et al. 2011. PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 2: comparative assessment of prediction methods of human volume of distribution. J Pharm Sci. 100(10):4074–4089.
  • Kirsten R, Nelson K, Kirsten D, Heintz B. 1998. Clinical pharmacokinetics of vasodilators. Part I. Clin Pharmacokinet. 34(6):457–482.
  • Korte S, Everitt J. 2019. The common marmoset in captivity and biomedical research. American College of Laboratory Animal Medicine. Cambridge (MA): Academic Press. Chapter 27. In: The use of the marmoset in toxicity testing and nonclinical safety assessment studies; p. 493–513.
  • Kusama T, Toda A, Shimizu M, Uehara S, Inoue T, Uno Y, Utoh M, Sasaki E, Yamazaki H. 2018. Association with polymorphic marmoset cytochrome P450 2C19 of in vivo hepatic clearances of chirally separated R-omeprazole and S-warfarin using individual marmoset physiologically based pharmacokinetic models. Xenobiotica. 48(10):1072–1077.
  • Layne DG, Power RA. 2003. Husbandry, handling, and nutrition for marmosets. Comp Med. 53(4):351–359.
  • Li Z, Wang G, Wang L-S, Zhang W, Tan Z-R, Fan L, Chen B-L, Li Q, Liu J, Tu J-H, et al. 2009. Effects of the CYP2C9*13 allele on the pharmacokinetics of losartan in healthy male subjects. Xenobiotica. 39(10):788–793.
  • Lo MW, Goldberg MR, McCrea JB, Lu H, Furtek CI, Bjornsson TD. 1995. Pharmacokinetics of losartan, an angiotensin II receptor antagonist, and its active metabolite EXP3174 in humans. Clin Pharmacol Ther. 58(6):641–649.
  • Mahmood I. 2010. Theoretical versus empirical allometry: facts behind theories and application to pharmacokinetics. J Pharm Sci. 99(7):2927–2933.
  • Matsumoto S, Uehara S, Kamimura H, Ikeda H, Maeda S, Hattori M, Nishiwaki M, Kato K, Yamazaki H. 2021. Human total clearance values and volumes of distribution of typical human cytochrome P450 2C9/19 substrates predicted by single-species allometric scaling using pharmacokinetic data sets in common marmosets genotyped for P450 2C19. Xenobiotica. 51(4):479–493.
  • McClellan KJ, Markham A. 1998. Telmisartan. Drugs. 56(6):1039–1044.
  • Miyamoto M, Iwasaki S, Chisaki I, Nakagawa S, Amano N, Hirabayashi H. 2017. Comparison of predictability for human pharmacokinetics parameters among monkeys, rats, and chimeric mice with humanised liver. Xenobiotica. 47(12):1052–1063.
  • Miyamoto M, Iwasaki S, Chisaki I, Nakagawa S, Amano N, Kosugi Y, Hirabayashi H. 2019. Prediction of human pharmacokinetics of long half-life compounds using chimeric mice with humanised liver. Xenobiotica. 49(12):1379–1387.
  • Mochizuki H, Murota N, Sato S, Nii K, Kouhei Y, Taniguchi M, Inoue R, Nishime C, Tsutsumi H. 2018. Approaches of validation of a 2-week combined repeated oral dose toxicity study with plasma micro sampling toxicokinetics (PMS-TK) in common marmosets. J Toxicol Sci. 43(11):685–695.
  • Nagilla R, Nord M, McAtee JJ, Jolivette LJ. 2011. Cassette dosing for pharmacokinetic screening in drug discovery: comparison of clearance, volume of distribution, half-life, mean residence time, and oral bioavailability obtained by cassette and discrete dosing in rats. J Pharm Sci. 100(9):3862–3874.
  • Nakada N. 2017. Evaluation of the utility of chimeric mice with humanized livers for the characterization and profiling of the metabolites of a selective inhibitor (YM543) of the sodium-glucose cotransporter 2. Pharm Res. 34(4):874–886.
  • Nakashima A, Kawashita H, Masuda N, Saxer C, Niina M, Nagae Y, Iwasaki K. 2005. Identification of cytochrome P450 forms involved in the 4-hydroxylation of valsartan, a potent and specific angiotensin II receptor antagonist, in human liver microsomes. Xenobiotica. 35(6):589–602.
  • Ohtawa M, Takayama F, Saitoh K, Yoshinaga T, Nakashima M. 1993. Pharmacokinetics and biochemical efficacy after single and multiple oral administration of losartan, an orally active nonpeptide angiotensin II receptor antagonist, in humans. Br J Clin Pharmacol. 35(3):290–297.
  • Orsi A, Rees D, Andreini I, Venturella S, Cinelli S, Oberto G. 2011. Overview of the marmoset as a model in nonclinical development of pharmaceutical products. Regul Toxicol Pharmacol. 59(1):19–27.
  • Poirier A, Cascais AC, Funk C, Lavé T. 2009. Prediction of pharmacokinetic profile of valsartan in humans based on in vitro uptake-transport data. Chem Biodivers. 6(11):1975–1987.
  • Prior H, Haworth R, Labram B, Roberts R, Wolfreys A, Sewell F. 2020. Justification for species selection for pharmaceutical toxicity studies. Toxicol Res (Camb)). 9(6):758–770.
  • Riede J, Poller B, Umehara K, Huwyler J, Camenisch G. 2016. New IVIVE method for the prediction of total human clearance and relative elimination pathway contributions from in vitro hepatocyte and microsome data. Eur J Pharm Sci. 86:96–102.
  • Ring BJ, Chien JY, Adkison KK, Jones HM, Rowland M, Jones RD, Yates JWT, Ku MS, Gibson CR, He H, et al. 2011. PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 3: comparative assessment of prediction methods of human clearance. J Pharm Sci. 100(10):4090–4110.
  • Schadt S, Bister B, Chowdhury SK, Funk C, Hop CECA, Humphreys WG, Igarashi F, James AD, Kagan M, Khojasteh SC, et al. 2018. A decade in the MIST: Learnings from investigations of drug metabolites in drug development under the “Metabolites in Safety Testing” regulatory guidance. Drug Metab Dispos. 46(6):865–878.
  • Smith D, Trennery P, Farningham D, Klapwijk J. 2001. The selection of marmoset monkeys (Callithrix jacchus) in pharmaceutical toxicology. Lab Anim. 35(2):117–130.
  • Smith DA, Beaumont K, Maurer TS, Li D. 2018. Relevance of half-life in drug design. J Med Chem. 61(10):4273–4282.
  • Soars MG, Riley RJ, Burchell B. 2001. Evaluation of the marmoset as a model species for drug glucuronidation. Xenobiotica. 31(12):849–860.
  • Son YW, Choi HN, Che JH, Kang BC, Yun JW. 2020. Advances in selecting appropriate non-rodent species for regulatory toxicology research: policy, ethical, and experimental considerations. Regul Toxicol Pharmacol. 116:104757.
  • Stangier J, Schmid J, Türck D, Switek H, Verhagen A, Peeters PA, van Marle SP, Tamminga WJ, Sollie FA, Jonkman JH. 2000a. Absorption, metabolism, and excretion of intravenously and orally administered [14C]telmisartan in healthy volunteers. J Clin Pharmacol. 40(12 Pt):1):1312–1322.
  • Stangier J, Su CA, Roth W. 2000b. Pharmacokinetics of orally and intravenously administered telmisartan in healthy young and elderly volunteers and in hypertensive patients. J Int Med Res. 28(4):149–167.
  • Sun P, Wang C, Liu Q, Meng Q, Zhang A, Huo X, Sun H, Liu K. 2014. OATP and MRP2-mediated hepatic uptake and biliary excretion of eprosartan in rat and human. Pharmacol Rep. 66(2):311–319.
  • Taavitsainen P, Kiukaanniemi K, Pelkonen O. 2000. In vitro inhibition screening of human hepatic P450 enzymes by five angiotensin-II receptor antagonists. Eur J Clin Pharmacol. 56(2):135–140.
  • Tenero D, Martin D, Ilson B, Jushchyshyn J, Boike S, Lundberg D, Zariffa N, Boyle D, Jorkasky D. 1998. Pharmacokinetics of intravenously and orally administered eprosartan in healthy males: absolute bioavailability and effect of food. Biopharm Drug Dispos. 19(6):351–356.
  • Tess DA, Eng H, Kalgutkar AS, Litchfield J, Edmonds DJ, Griffith DA, Varma MVS. 2020. Predicting the human hepatic clearance of acidic and zwitterionic drugs. J Med Chem. 63(20):11831–11844.
  • Uehara S, Uno Y, Inoue T, Kawano M, Shimizu M, Toda A, Utoh M, Sasaki E, Yamazaki H. 2016. Individual differences in metabolic clearance of S-warfarin efficiently mediated by polymorphic marmoset cytochrome P450 2C19 in livers. Drug Metab Dispos. 44(7):911–915.
  • Uno Y, Uehara S, Inoue T, Kawamura S, Murayama N, Nishikawa M, Ikushiro S, Sasaki E, Yamazaki H. 2020. Molecular characterization of functional UDP-glucuronosyltransferases 1A and 2B in common marmosets. Biochem Pharmacol. 172:113748.
  • Wajima T, Yano Y, Fukumura K, Oguma T. 2004. Prediction of human pharmacokinetic profile in animal scale up based on normalizing time course profiles. J Pharm Sci. 93(7):1890–1900.
  • Waldmeier F, Flesch G, Müller P, Winkler T, Kriemler HP, Bühlmayer P, De Gasparo M. 1997. Pharmacokinetics, disposition and biotransformation of [14C]-radiolabelled valsartan in healthy male volunteers after a single oral dose. Xenobiotica. 27(1):59–71.
  • White RE, Manitpisitkul P. 2001. Pharmacokinetic theory of cassette dosing in drug discovery screening. Drug Metab Dispos. 29(7):957–966.
  • Williamson KM, Patterson JH, McQueen RH, Adams KF Jr, Pieper JA. 1998. Effects of erythromycin or rifampin on losartan pharmacokinetics in healthy volunteers. Clin Pharmacol Ther. 63(3):316–323.
  • Yamada A, Maeda K, Ishiguro N, Tsuda Y, Igarashi T, Ebner T, Roth W, Ikushiro S, Sugiyama Y. 2011. The impact of pharmacogenetics of metabolic enzymes and transporters on the pharmacokinetics of telmisartan in healthy volunteers. Pharmacogenet Genomics. 21(9):523–530.
  • Yamashiro W, Maeda K, Hirouchi M, Adachi Y, Hu Z, Sugiyama Y. 2006. Involvement of transporters in the hepatic uptake and biliary excretion of valsartan, a selective antagonist of the angiotensin II AT1-receptor, in humans. Drug Metab Dispos. 34(7):1247–1254.
  • Zaidenstein R, Soback S, Gips M, Avni B, Dishi V, Weissgarten Y, Golik A, Scapa E. 2001. Effect of grapefruit juice on the pharmacokinetics of losartan and its active metabolite E3174 in healthy volunteers. Ther Drug Monit. 23(4):369–373.
  • Zühlke U, Weinbauer G. 2003. The common marmoset (Callithrix jacchus) as a model in toxicology. Toxicol Pathol. 31(Suppl):123–127.