Summary of the National Institute of Child Health and Human Development-Best Pharmaceuticals for Children Act Pediatric Formulation Initiatives Workshop-Pediatric Biopharmaceutics Classification System Working Group

Clinical Therapeutics

Volumn 34, Issue 11, 2012, Pages

  Abdel Rahman, Susan M ^a   Amidon, Gordon L ^b   Kaul, Ajay ^c,e   Lukacova, Viera ^d   Vinks, Alexander A ^c,e   Knipp, Gregory T ^f  

^a CHILDREN S MERCY HOSPITAL   (United States)

^b UNIVERSITY OF MICHIGAN   (United States)

^c CINCINNATI CHILDREN'S HOSPITAL MEDICAL CENTER   (United States)

^d Simulations Plus Inc   (United States)

^e UNIVERSITY OF CINCINNATI COLLEGE OF MEDICINE   (United States)

^f PURDUE UNIVERSITY   (United States)

Author keywords

Biorepository; Drug metabolizing enzymes; Gastroinestinal physiology; Ontogeny; PBPK; Pediatric biopharmaceutics classification system

Indexed keywords

AMOXICILLIN; AZITHROMYCIN; BREAST CANCER RESISTANCE PROTEIN; CARBAMAZEPINE; CEFDINIR; CYTOCHROME P450 1A2; CYTOCHROME P450 2B6; CYTOCHROME P450 2C19; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 2E1; CYTOCHROME P450 3A4; CYTOCHROME P450 3A5; CYTOCHROME P450 3A7; DRUG METABOLIZING ENZYME; GLUCURONOSYLTRANSFERASE; METHYLPHENIDATE; MIDAZOLAM; MULTIDRUG RESISTANCE PROTEIN; MULTIDRUG RESISTANCE PROTEIN 1; MULTIDRUG RESISTANCE PROTEIN 5; OMEPRAZOLE; PARACETAMOL; PHENOBARBITAL; SULFOTRANSFERASE; VALACICLOVIR;

BREAST FEEDING; CANADA; DIGESTIVE FUNCTION; DRUG DISPOSITION; DRUG EXCRETION; DRUG FORMULATION; DRUG METABOLISM; DRUG TRANSPORT; EPITHELIUM CELL; GASTROINTESTINAL TRACT; GASTROINTESTINAL TRANSIT; HUMAN; INTESTINE ABSORPTION; INTESTINE MUCOSA PERMEABILITY; INTESTINE TRANSIT TIME; INTUBATION; KNOWLEDGE; MEDICAL SOCIETY; NATIONAL HEALTH ORGANIZATION; ONTOGENY; PEDIATRIC BIOPHARMACEUTICS CLASSIFICATION SYSTEM WORKING GROUP; PROTEIN EXPRESSION; PROTEIN FUNCTION; REVIEW; STUDY DESIGN; TELECONFERENCE; UNITED STATES; WORKSHOP;

ADOLESCENT; AGE FACTORS; AGING; BIOMEDICAL RESEARCH; BIOTRANSFORMATION; CHEMISTRY, PHARMACEUTICAL; CHILD; CHILD, PRESCHOOL; GASTROINTESTINAL TRACT; HUMANS; INFANT; INFANT, NEWBORN; MODELS, BIOLOGICAL; NATIONAL INSTITUTE OF CHILD HEALTH AND HUMAN DEVELOPMENT (U.S.); PEDIATRICS; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS; TECHNOLOGY, PHARMACEUTICAL; TERMINOLOGY AS TOPIC; TISSUE BANKS; UNITED STATES;

EID: 84869048695     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/j.clinthera.2012.09.014     Document Type: Review

References (73)

1. Kramer S.D. Why and how pharmacokinetics change from birth to adolescence: an introduction. Bull Tech Gattefossé 2009, 102:9-18.
2. Bartelink I.H., Rademaker C.M., Schobben A.F., van den Anker J.N. Guidelines on paediatric dosing on the basis of developmental physiology and pharmacokinetic considerations. Clin Pharmacokinet 2006, 45:1077-1097.
3. Kearns G.L. Ontogeny and drug biotransformation: the intersection of pharmacogenetics and development. Bull Tech Gattefossé 2009, 102:19-28.
4. Rose K. Challenges in pediatric drug development: a pharmaceutical industry perspective. Pediatr Drugs 2009, 11:57-59.
5. U.S. Food and Drug Administration, Pediatric Product Development, Accessed September 2, 2012. http://www.fda.gov/Drugs/DevelopmentApprovalProcess/DevelopmentResources/ucm049867.htm.
6. Zajicek A. The National Institutes of Health and the Best Pharmaceuticals for Children Act. Pediatr Drugs 2009, 11:45-47.
7. Thompson K.C. Extemporaneous formulations: comparison with labeled pediatric formulations. Am Pharm Rev 2010, 53-55. April/March.
8. Milne C.P., Bruss J.B. The economics of pediatric formulation development for off-patent drugs. Clin Ther 2008, 30:2133-2145.
9. Shirkey H. Editorial commentary: therapeutic orphans. J Pediatr 1968, 72:119-120.
10. 2000, Waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a Biopharmaceutics Classification System; FDA guidance for industry, Federal Drug and Food Administration, Rockville, MD, Accessed September 2, 2012. http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm070246.pdf.
11. Amidon G.L., Lennernas H., Shah V.P., Crison J.R. A theoretical basis for a Biopharmaceutics Drug Classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995, 12:413-420.
12. Yu L.X., Amidon G.L., Polli G.L., et al. Biopharmaceutics Classification System: the scientific basis for biowaiver extensions. Pharm Res 2002, 19:921-925.
13. Kaus L.C., Gillespie W.R., Hussain A.S., Amidon G.L. The effect of in vivo dissolution, gastric emptying rate, and intestinal transit time on the peak concentration and area-under-the-curve of drugs with different gastrointestinal permeabilities. Pharm Res 1999, 16:272-280.
14. Martinez M.N., Amidon G.L. A mechanistic approach to understanding the factors affecting drug absorption: a review of fundamentals. J Clin Pharmacol 2002, 42:620-643.
15. Newman A., Knipp G., Zografi G. Assessing the performance of amorphous solid dispersions. J Pharm Sci 2012, 101:1355-1377.
16. Kalász H., Antal I. Drug excipients. Curr Med Chem 2006, 13:2535-2563.
17. Wu C.Y., Benet L.Z. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res 2005, 22:11-23.
18. Benet L.Z., Broccatelli F., Oprea T.I. BDDCS applied to over 900 drugs. AAPS J 2011, 13:519-547.
19. Broccatelli F., Cruciani G., Benet L.Z., Oprea T.I. BDDCS class prediction for new molecular entities. Mol Pharm 2012, 9:570-580.
20. Dickinson C. Development of gastric secretory function. Fetal and Neonatal Physiology 1998, 1364-1372. W.B. Saunders Company, Philadelphia, PA. 2nd ed. R.A. Polin, W.W. Fox (Eds.).
21. Koldovsky O. Digestive-absorption functions in fetuses, infants, and children. Fetal and Neonatal Physiology 1998, 1400-1418. W.B. Saunders Company, Philadelphia, PA. 2nd ed. R.A. Polin, W.W. Fox (Eds.).
22. Anderson G.D., Lynn A.M. Optimizing pediatric dosing: a developmental pharmacologic approach. Pharmacotherapy 2009, 29:680-690.
23. Cohen M.B. Absorption and secretion of electrolytes and fluid by the intestine. Perinatal and Pediatric Pathophysiology: A Clinical Perspective 1993, 401-411. Edward Arnold, A Division of Hodder & Stoughton, Suffolk, UK. 1st ed. P.D. Gluckman, M.A. Heymann (Eds.).
24. Ross A. Organogenesis, innervations, and histologic development of the gastrointestinal tract. Fetal and Neonatal Physiology 1998, 1342-1353. W.B. Saunders Company, Philadelphia, PA. 2nd ed. R.A. Polin, W.W. Fox (Eds.).
25. Pácha J. Development of intestinal transport function in mammals. Physiol Rev 2000, 80:1633-1667.
26. Gupta M., Brans Y.W. Gastric retention in neonates. Pediatrics 1978, 62:26-29.
27. Seibert J.J., Byrne W.J., Euler A.R. Gastric emptying in children: unusual patterns detected by scintigraphy. AJR Am J Roentgenol 1983, 141:49-51.
28. Weaver L.T., Austin S., Cole T.J. Small intestinal length: a factor essential for gut adaptation. Gut 1991, 32:1321-1323.
29. Omari T.I., Rudolph C.D. Chapter 125: Gastrointestinal motility. Fetal and Neonatal Physiology 1998, 1373-1383. W.B. Saunders Company, Philadelphia, PA. 2nd ed. R.A. Polin, W.W. Fox (Eds.).
30. Desso J.M., Williams A.L. Contrasting the gastrointestinal tracts of mammals: factors that influence absorption. Ann Rep Med Chem 2008, 43:353-371.
31. De Wildt S.N., Kearns G.L., Leeder J.S., Van Den Anker J.N. Cytochrome P450 3A. Clin Pharmacokinet 1999, 37:485-505.
32. Kearns G.L., Abdel-Rahman S.M., Alander S.W., et al. Developmental pharmacology - drug disposition, action, and therapy in infants and children. N Engl J Med 2003, 349:1157-1167.
33. Tucker G.T. Developmental pharmacokinetics/pharmacodynamics-what have we learnt?. Bul Tech Gattefossé 2009, 102:29-40.
34. Johnson T. The development of drug metabolising enzymes and their influence on the susceptibility to adverse drug reactions in children. Toxicology 2003, 192:37-48.
35. Payne K., Mattheyse F.J., Liebenberg D., Dawes T. The pharmacokinetics of midazolam in paediatric patients. Clin Pharmacol 1989, 37:267-272.
36. Miyagi S.J., Milne A.M., Coughtrie M.W.H., Collier A.C. The neonatal development of hepatic UGT1A9: implications of pediatric pharmacokinetics. Drug Metab Dispos 2012, 40:1321-1327.
37. Zaya M.J., Hines R.N., Stevens J.C. Epirubicin glucuronidation and UGT2B7 developmental expression. Drug Metab Dispos 2006, 34:2097-2101.
38. Miyagi S.J., Collier A.C. Pediatric development of glucuronidation: the ontogeny of hepatic UGT1A4. Drug Metab Dispos 2007, 35:1587-1592.
39. Miyagi S.J., Collier A.C. The development of UDP-glucuronosyltransferases 1A1 and 1A6 in the pediatric liver. Drug Metab Dispos 2011, 39:912-919.
40. Alcorn J., McNamara P.J. Ontogeny of hepatic and renal systemic clearance pathways in infants: part I. Clin Pharmacokinet 2002, 41:959-998.
41. Fakhoury M., Litalien C., Medard Y., et al. Localization and mRNA expression of CYP3A and P-glycoprotein in human duodenum as a function of age. Drug Metab Dispos 2005, 33:1603-1607.
42. Johnsrud E.K., Koukouritaki S.B., Divakaran K., et al. Human hepatic CYP2E1 expression during development. J Pharm Exp Ther 2003, 307:402-407.
43. Koukouritaki S.B., Manro J.R., Marsh S.A., et al. Developmental expression of human hepatic CYP2C9 and CYP2C19. J Pharm Exp Ther 2004, 308:965-974.
44. Stevens J.C., Hines R.N., Gu C., et al. Developmental expression of the major human hepatic CYP3A enzymes. J Pharm Exp Ther 2003, 307:573-582.
45. Lacroix D., Sonnier M., Moncion A., et al. Expression of CYP3A in the human liver: evidence that the shift between CYP3A7 and CYP3A4 occurs immediately after birth. Eur J Biochem 1997, 247:625-634.
46. Sonnier M., Cresteil T. Delayed ontogenesis of CYP1A2 in the human liver. Eur J Biochem 1998, 251:893-898.
47. Treluyer J.-M., Jacqz-Aigrain E., Alvarez F., Cresteil T. Expression of CYP2D6 in developing human liver. Eur J Biochem 1991, 202:583-588.
48. Treluyer J.-M., Gueret G., Cheron G., et al. Developmental expression of CYP2C and CYP2C-dependent activities in the human liver: in-vivo/in-vitro correlation and inducibility. Pharmacogenetics 1997, 7:441-452.
49. Vieira I., Sonnier M., Cresteil T. Developmental expression of CYP2E1 in the human liver: hypermethylation control of gene expression during the neonatal period. Eur J Biochem 1996, 238:476-483.
50. Alcorn J., McNamara P.J. Ontogeny of hepatic and renal systemic clearance pathways in infants: part II. Clin Pharmacokinet 2002, 41:1077-1094.
51. Blanco J.G., Harrison P.L., Evans W.E., Relling M.V. Human cytochrome P450 maximal activities in pediatric versus adult liver. Drug Metab Dispos 2000, 28:379-382.
52. Buddington R.K. Intestinal nutrient transport during ontogeny of vertebrates. Am J Physiol Reg Integrative Comp Physiol 1992, 263:503-509.
53. Buddington R.K., Diamond J.M. Ontogenetic development of intestinal nutrient transporters. Ann Rev Physiol 1989, 51:601-619.
54. Sherwin C.M., Saldaña S.N., Bies R.R., et al. Population pharmacokinetic modeling of risperidone and 9-hydroxyrisperidone to estimate CYP2D6 subpopulations in children and adolescents. Ther Drug Monit 2012, 34:535-544.
55. Zuppa A.F., Nicolson S.C., Barrett J.S., Gastonguay M.R. Population pharmacokinetics of pentobarbital in neonates, infants, and children after open heart surgery. J Pediatr 2011, 159:414-419. e1-3.
56. de Wildt S.N., de Hoog M., Vinks A.A., et al. Population pharmacokinetics and metabolism of midazolam in pediatric intensive care patients. Crit Care Med 2003, 31:1952-1958.
57. Vinks A.A. Important role of population pharmacokinetic/pharmacodynamic modeling in pediatric therapeutics. J Pediatr 2011, 159:361-363.
58. Parrott N., Lukacova V., Fraczkiewicz G., Bolger M.B. Predicting pharmacokinetics of drugs using physiologically based modeling-application to food effects. AAPS J 2009, 11:45-53.
59. Bolger M.B., Lukacova V., Woltosz W.S. Simulations of the nonlinear dose dependence for substrates of influx and efflux transporters in the human intestine. AAPS J 2009, 11:353-363.
60. Johnson T.N., Rostami-Hodjegan A. Resurgence in the use of physiologically based pharmacokinetic models in pediatric clinical pharmacology: parallel shift in incorporating the knowledge of biological elements and increased applicability to drug development and clinical practice. Paediatr Anaesth 2011, 21:291-301.
61. Edginton A.N. Knowledge-driven approaches for the guidance of first-in-children dosing. Paediatr Anaesth 2011, 21:206-213.
62. Parrott N., Davies B., Hoffmann G., et al. Development of a physiologically based model for oseltamivir and simulation of pharmacokinetics in neonates and infants. Clin Pharmacokinet 2011, 50:613-623.
63. Cytochrome P450 Drug Interaction Table. Indianapolis. IN: Division of Clinical Pharmacology 2009, Indiana University School of Medicine, Accessed September 2, 2012. http://medicine.iupui.edu/clinpharm/ddis/table.aspx.
64. Laine J.E., Auriola S., Pasanen M., Juvonen R.O. Acetaminophen bioactivation by human cytochrome P450 enzymes and animal microsomes. Xenobiotica 2009, 39:11-21.
65. Dahan A., Miller J.M., Amidon G.L. Prediction of solubility and permeability class membership: provisional BCS classification of the world's top oral drugs. AAPS J 2009, 11:740-746.
66. Therapeutic Systems Research Laboratories, Inc. (TSRL) searchable database for U.S. human BCS classification Accessed September 1, 2012. http://69.20.123.154/services/bcs/search.cfm.
67. Kim J.S., Mitchell S., Kijek P., et al. The suitability of an in situ perfusion model for permeability determinations: utility for BCS class I biowaiver requests. Mol Pharm 2006, 3:686-694.
68. Babic Z., Svoboda-Beusan I., Kucisec-Tepes N., et al. Increased activity of Pgp multidrug transporter in patients with Helicobacter pylori infection. World J Gastroenterol 2005, 11:2720-2725.
69. Bertilsson L., Tybring G., Widén J., et al. Carbamazepine treatment induces the CYP3A4 catalysed sulphoxidation of omeprazole, but has no or less effect on hydroxylation via CYP2C19. Br J Clin Pharmacol 1997, 44:186-189.
70. Abelö A., Andersson T.B., Antonsson M., et al. Stereoselective metabolism of omeprazole by human cytochrome P450 enzymes. Drug Metab Dispos 2000, 28:966-972.
71. Kim I., Chu X.Y., Kim S., et al. Identification of a human valacyclovirase: biphenyl hydrolase-like protein as valacyclovir hydrolase. J Biol Chem 2003, 278:25348-25356.
72. Kulo A., de Hoon J.N., Allegaert K. The propylene glycol research project to illustrate the feasibility and difficulties to study toxicokinetics in neonates. Int J Pharm 2012, 435:112-114.
73. Custodio J.M., Wu C.Y., Benet L.Z. Predicting drug disposition absorption/elimination and the role of food on drug absorption. Adv Drug Deliv Rev 2008, 60:717-733.