Prof. Bialer
Key Words: Pharmacokinetics (PK), PK-based design of drugs, antiepileptics, CNS drugs, chirality.
Scientific Interest:
Pharmacokinetics and biopharmaceutics of existing and new drugs.
Pharmacokinetic-based design of new antiepileptics and CNS drugs.
Structure-pharmacokinetic-pharmacodynamic relationships (SPPR).
Pharmacokinetic evaluation of drug interactions, new drug delivery systems, prodrugs and controlled-release formulations.
Stereospecific pharmacokinetic and pharmacodynanmic analysis of chiral drugs
Industry
Various international pharmaceutical companies
Collaborations
NIH Epilepsy Branch
Prof. Rene H. Levy, Univ. of Washington, Seattle, USA
Prof. H. Steve White, Univ. of Utah, USA
Drs. Bert de Boer and Rob Voskyl, Leiden Univ.,Holland
Prof. Emilio Perucca, Univ. of Pavia, Italy
Prof. Richard Finell, Texas A&M Univ. ,USA
Laboratory Techniques
Pharmacokinetic (PK) analysis
PK-based synthesis and design
Analytical chemistry GC-MS, LC-MS, HPLC, GC
Metabolic Studies
Patents:
M Bialer, S Hadad, J Herzig, JSterling, D Lerner, M Shirvan. Derivatives of valproic acid amide and 2-valproenoic acid amides, methods of making and use thereof as anticonvulsant agent. U.S. Patnet No. 5,585,358 Issued 17.12.1996.
1. J Sterling, 1. Y Herzig, M Bialer, 1. A Haj-Yehia, B Yagen, . Derivatives of tetra methylcyclopropane. U.S. Patnet No. 5,880,157. Issued 9. 3.1999.
M Bialer, A Dagan, S Sussan. Anticonvulsant drugs and pharmaceutical compositions thereof. U.S. Patent No. 6,028,102. Issued 22.2.2000.
M Bialer, B Yagen, N Papo. Active derivative of valproic acid for the treatment of neurological and psychotic disorders and a method for their preparation. U.S. Patent No. 6,323,365. Issued 27.11.01.
A Sintov, A Volosov, M Bialer, B Yagen. Pharmaceutical compositions containing low-melting waxes. U.S. Pat Applic Ser 09/743,260. Filing 1.1.01.
Sample of recent research publications:
S Sussan, A Dagan, S Blotnik, M Bialer. Structural requirements for the design of antiepileptic-glycine derivatives. Epilepsy Res. 34:207-220 (1999).
M Roeder, V Schurig, O Spiegelstein, M Bialer, B. Yagen. Absolute configuration of the four stereoisomers of valnoctamide (2-ethyl-3-methyl valeramide), a potential new stereospecific antiepileptic and CNS drug. Tetrahedron: Asymmetr.10:841-853 (1999).
M Bialer. Pharmacokinetic considerations in the design of better and safer new antiepileptic drugs. J. Control. Release, 62:187-192 (1999).
A Volosov, S Xiandong, . Perucca, B Yagen, A Sintov, M Bialer. Enantioselective pharmacokinetics of 10-hydroxy carbazepine following oral administration of oxcarbazepine to healthy Chinese subjects. Clin. Pharmacol. Ther. 66:547-553 (1999).
O Spiegelstein, DL Kroetz, RH Levy, B Yagen, SI Hurst, M Levi, A Haj-Yehia, M. Bialer. Structure activity relationships of human microsomal epoxide hydroalse inhibition by amide and acid analogues of valproic acid. Pharm. Res. 17:216-221 (2000).
H Lindekens, I Smolders, GM Khan, M Bialer, G Ebinger, Y Michotte. In vivo study of the effect of valpromide and valnoctamide in the pilocarpine rat model of focal epilepsy. Pharm. Res. 17:1408-1413 (2000).
M Bialer, SJ Johannessen, HJ Kupferberg, RH Levy, P Loiseau, E Perucca. Progress report on new antiepileptic drugs: A summary of the Fifth Eilat Conference (EILAT V). Epilepsy Res. 43:11-58 (2001).
M Wasserman, B Yagen, S Blotnik, N Pappo, M Bialer. Stereoselective pharmacokinetic analysis and antiepileptic activity of N-2-hydroxypropyl valpromide, a chiral central nerve system-active valproylamide. Ther. Drug Monit., 23:414-420 (2001).
N Isoherranen, B Yagen, S Soback, M Roeder, V Schurig , M Bialer. Pharmacokinetic analysis of levetiracetam and its enantiomer R-alpha-ethyl-2-oxo-pyrrolidine acetamide in dogs. Epilepsia 42:825-830 (2001).
N Isoherranen, JH Woodheard, HS White, M Bialer. Anticonvulsant profile of valrocemide (TV 1901): A new antiepileptic and CNS drug. Epilepsia 42:831-836 (2001).
M Bialer. New antiepileptic drugs currently in clinical trials. Is there a strategy in their development? Ther. Drug Monit., 24:85-90 (2002).
