Translational model to predict pulmonary pharmacokinetics and efficacy in man for inhaled bronchodilators

CPT: Pharmacometrics and Systems Pharmacology

Volumn 7, Issue 3, 2018, Pages 147-157

  Hendrickx, Ramon ^a   Bergström, Eva Lamm ^a   Janzén, David L I ^a   Fridén, Markus ^a   Eriksson, Ulf ^a   Grime, Ken ^a   Ferguson, Douglas ^b  

^a ASTRAZENECA R AND D   (Sweden)

^b ASTRAZENECA   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

BRONCHODILATING AGENT; FORMOTEROL; GLYCOPYRRONIUM; INDACATEROL; IPRATROPIUM BROMIDE; SALBUTAMOL; SALMETEROL; TIOTROPIUM BROMIDE;

ARTICLE; DRUG DISTRIBUTION; DRUG EFFICACY; FORCED EXPIRATORY VOLUME; HUMAN; HUMAN EXPERIMENT; IC50; LUNG PARENCHYMA; MALE; MAXIMUM PLASMA CONCENTRATION; PHARMACODYNAMICS; PHARMACOKINETIC PARAMETERS; PRIORITY JOURNAL; ANIMAL; ANIMAL MODEL; BIOLOGICAL MODEL; DOG; INHALATIONAL DRUG ADMINISTRATION; INTRAVENOUS DRUG ADMINISTRATION; LUNG; PHYSIOLOGY; PRECLINICAL STUDY; RAT; SPRAGUE DAWLEY RAT;

ADMINISTRATION, INHALATION; ADMINISTRATION, INTRAVENOUS; ANIMALS; BRONCHODILATOR AGENTS; DOGS; DRUG EVALUATION, PRECLINICAL; FORCED EXPIRATORY VOLUME; HUMANS; LUNG; MALE; MODELS, ANIMAL; MODELS, BIOLOGICAL; RATS; RATS, SPRAGUE-DAWLEY;

EID: 85044469406     PISSN: None     EISSN: 21638306     Source Type: Journal    
DOI: 10.1002/psp4.12270     Document Type: Article

References (34)

1. Tayab, Z.R. & Hochhaus, G. Pharmacokinetic/pharmacodynamic evaluation of inhalation drugs: application to targeted pulmonary delivery systems. Expert Opin. Drug Deliv. 2, 519-532 (2005).
2. Borghardt, J.M., Weber, B., Staab, A. & Kloft, C. Pharmacometric models for characterizing the pharmacokinetics of orally inhaled drugs. AAPS J. 17, 853-870 (2015).
3. Ericsson, T., Fridén, M., Kärrman-Mardh, C., Dainty, I. & Grime, K. Benchmarking of human dose prediction for inhaled medicines from preclinical in vivo data. Pharm. Res. (2017).
4. Wu, K., Looby, M., Pillai, G., Pinault, G., Drollman, A.F. & Pascoe, S. Population pharmacodynamic model of the longitudinal FEV1 response to an inhaled long-acting anti-muscarinic in COPD patients. J. Pharmacokinet. Pharmacodyn. 38, 105-119 (2011).
5. Nielsen, J.C., Hutmacher, M.M., Cleton, A., Martin, S.W. & Ribbing, J. Longitudinal FEV1 dose-response model for inhaled PF-00610355 and salmeterol in patients with chronic obstructive pulmonary disease. J. Pharmacokinet. Pharmacodyn. 39, 619-634 (2012).
6. Gaz, C., Cremona, G., Panunzi, S., Patterson, B. & De Gaetano, A. A geometrical approach to the PKPD modelling of inhaled bronchodilators. J. Pharmacokinet. Pharmacodyn. 39, 415-428 (2012).
7. Agoram, B.M., Milligan, P.A. & van der Graaf, P.H. A non-parametric method to analyse time-course of effect in the absence of pharmacokinetic data: application to inhaled bronchodilators. Eur. J. Pharm. Sci. 34, 250-256 (2008).
8. Bäckström, E., Boger, E., Lundqvist, A., Hammarlund-Udenaes, M. & Fridén, M. Lung retention by lysosomal trapping of inhaled drugs can be predicted in vitro with lung slices. J. Pharm. Sci. 105, 3432-3439 (2016).
9. Cooper, A.E., Ferguson, D. & Grime, K. Optimisation of DMPK by the inhaled route: challenges and approaches. Curr. Drug Metab. 13, 457-473 (2012).
10. Jones, R.M. & Harrison, A. A new methodology for predicting human pharmacokinetics for inhaled drugs from oratracheal pharmacokinetic data in rats. Xenobiotica 42, 75-85 (2012).
11. Shaw, D.E. et al. Optimization of platelet-derived growth factor receptor (PDGFR) inhibitors for duration of action, as an inhaled therapy for lung remodeling in pulmonary arterial hypertension. J. Med. Chem. 59, 7901-7914 (2016).
12. Wenlock, M.C., Austin, R.P., Potter, T. & Barton, P. A highly automated assay for determining the aqueous equilibrium solubility of drug discovery compounds. J. Lab. Autom. 16, 276-284 (2011).
13. Wenlock, M.C., Potter, T., Barton, P. & Austin, R.P. A method for measuring the lipophilicity of compounds in mixtures of 10. J. Biomol. Screen. 16, 348-355 (2011).
14. Wan, H. et al. High-throughput screening of pKa values of pharmaceuticals by pressure-assisted capillary electrophoresis and mass spectrometry. Rapid Commun. Mass Spectrom. 17, 2639-2648 (2003).
15. Walland, A., Palluk, R., Burkard, S. & Hammer, R. Compensation of muscarinic bronchial effects of talsaclidine by concomitant sympathetic activation in guinea pigs. Eur. J. Pharmacol. 330, 213-219 (1997).
16. Bäckström, E. et al. Development of a novel lung slice methodology for profiling of inhaled compounds. J. Pharm. Sci. 105, 838-845 (2016).
17. Davies, B. & Morris, T. Physiological parameters in laboratory animals and humans. Pharm. Res. 10, 1093-1095 (1993).
18. Gabrielsson, J. & Weiner, D. Pharmacokinetic and Pharmacodynamic Data Analysis, 5th edn. (Stockholm, Sweden, Swedish Pharmaceutical Press, 2017).
19. Stocks, M.J. et al. Discovery of AZD3199, an inhaled ultralong acting b2 receptor agonist with rapid onset of action. ACS Med. Chem. Lett. 5, 416-421 (2014).
20. Lindén, A., Bergendal, A., Ullman, A., Skoogh, B.E. & Löfdahl, C.G. Salmeterol, formoterol, and salbutamol in the isolated guinea pig trachea: differences in maximum relaxant effect and potency but not in functional antagonism. Thorax 48, 547-553 (1993).
21. Molimard, M., Naline, E., Zhang, Y., Le Gros, V., Begaud, B. & Advenier, C. Longand short-acting beta2 adrenoceptor agonists: interactions in human contracted bronchi. Eur. Respir. J. 11, 583-588 (1998).
22. Naline, E., Trifilieff, A., Fairhurst, R.A., Advenier, C. & Molimard, M. Effect of indacaterol, a novel long-acting beta2-agonist, on isolated human bronchi. Eur. Respir. J. 29, 575-581 (2007).
23. Cazzola, M. et al. Pharmacological characterization of the interaction between aclidinium bromide and formoterol fumarate on human isolated bronchi. Eur. J. Pharmacol. 745, 135-143 (2014).
24. Cazzola, M. et al. Pharmacological characterisation of the interaction between glycopyrronium bromide and indacaterol fumarate in human isolated bronchi, small airways and bronchial epithelial cells. Respir. Res. 17, 70 (2016).
25. Villetti, G. et al. Pharmacological assessment of the duration of action of glycopyrrolate vs tiotropium and ipratropium in guinea-pig and human airways. Br. J. Pharmacol. 148, 291-298 (2006).
26. Hughes, A.D. et al. Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-inclass dual pharmacology multivalent muscarinic antagonist and b2 agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD). J. Med. Chem. 58, 2609-2622 (2015).
27. Borghardt, J.M., Weber, B., Staab, A., Kunz, C. & Kloft, C. Model-based evaluation of pulmonary pharmacokinetics in asthmatic and COPD patients after oral olodaterol inhalation. Br. J. Clin. Pharmacol. 82, 739-753 (2016).
28. Bartels, C., Looby, M., Sechaud, R. & Kaiser, G. Determination of the pharmacokinetics of glycopyrronium in the lung using a population pharmacokinetic modelling approach. Br. J. Clin. Pharmacol. 76, 868-879 (2013).
29. Hendrickx, R. et al. Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2. J. Med. Chem. 56, 7232-7242 (2013).
30. Koepsell, H., Lips, K. & Volk, C. Polyspecific organic cation transporters: structure, function, physiological roles, and biopharmaceutical implications. Pharm. Res. 24, 1227-1251 (2007).
31. Anderson, G.P., Lindén, A. & Rabe, K.F. Why are long-acting beta-adrenoceptor agonists long-acting? Eur. Respir. J. 7, 569-578 (1994).
32. Jacobsen, J.R. Third-generation long-acting b2-adrenoceptor agonists: medicinal chemistry strategies employed in the identification of once-daily inhaled b2-adrenoceptor agonists. Future Med. Chem. 3, 1607-1622 (2011).
33. Vauquelin, G. & Charlton, S.J. Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action. Br. J. Pharmacol. 161, 488-508 (2010).
34. Boger, E. et al. Systems pharmacology approach for prediction of pulmonary and systemic pharmacokinetics and receptor occupancy of inhaled drugs. CPT Pharmacometrics Syst. Pharmacol. 5, 201-210 (2016).