We have an active research program covering a wide range of topics related to oral and parenteral drug delivery. Listed below are selected references and patents describing work that has been done in our laboratories and those of our collaborators:
Nieman M, Burke F, Warnock M, Zhou Y, Sweigart J, Chen A, Ricketts D, Lucchesi B, Chen Z, DiCera E, Hilfinger J, Kim JS, Mosberg H, Schmaier A. Thrombostatin FM Compounds: Direct Thrombin Inhibitors–Mechanism of Action In Vitro and In Vivo. Accepted for publication J Thrombosis Haemostasis, Feb (2008).
Peterson L, Kashemirov B, Ericksson U, Kim JS, Mithcell S, Kijek P, Lee KD, Hilfinger J, McKenna J. Serine Side-Chain-Linked Peptidomimetic Prodrugs of Cidofovir and Cyclic cidofovir: C-Ester Effects on Transport and Activation. 21st ICAR Annual Conference (2008) A46 (77).
Breitenbach J, Shen W, Hilfinger J, Drach J. Synthesis and Activity of Vidarabine D-Amino Acid Prodrugs as Potential Pox Virus Agents. 21st ICAR Annual Conference (2008) A54 (99).
Gentry B, Shen W, Breitenbach J, Hilfinger J, Drach J. Vidarabine Prodrugs as Potential Inhibitors of Adenosine Deaminase. 21st ICAR Annual Conference (2008) A56 (103).
Schmaier AH, Burke F, Warnock M, Nieman M, Hilfinger J, Mosberg H. Thrombostatin FM19-A Thrombin Receptor Activation Antagonist. J Thromb Haemost (2007): 5 Supplement 2; P-M-351.
Mittal S., Tsume Y., Landowski CP., Lee KD., Hilfinger JM., Amidon GL. Proline prodrug of melphalan, prophalan-1, demonstrates high therapeutic index in a murine melanoma model. Eur J Pharm Biopharm (2007) Nov; 67(3) 752-8 Epub (2007) Apr.4.
Peterson LW., Kashemirov BA., Blazewska KM., Breitenback J., Borysko K., Drach JC., Kim J-S., Kijek P, Hilfinger JM., McKenna CE. Synthesis and Structure – Activity Aspects of Some Cyclic Cidofovir Peptidomimetic Prodrugs. 20th International Conference on Antiviral Research ICAR 74(3) (2007) A33.
Peterson L, Kashemirov B, Saejueng K, Breitenbach J, Borysko K, Drach J, Kim JS, Kijek P, Mitchell S, Hilfinger J, McKenna C. Novel Synthetic Approaches to Cidofovir and Foscarnet Prodrugs. 20th International conference on Antiviral Research ICAR (2007) A74 (114).
McKenna CE., Kashemirov BA, Peterson LW., Eriksson U, Kim J-S, Mitchell S, Kijek P, Hilfinger JM, Drach JC, Cidofovir and Foscarnet Peptide Prodrugs, 19th International Conference on Antiviral Research, ICAR, (2006).
Wu JZ., Breitenbach J., Eriksson U., Hilfinger JM., Drach JC., Amidon GL., Amino acid ester prodrugs of Vidarabine: Stability, permeability and activity against vaccinia virus. 19th international Conference on Antiviral Research ICAR. A59 (136) (2006).
Eriksson, U., Peterson, L.W., Kim, J.S., Mitchell, S., Kijek, P., Hilfinger, J.M., Drach, J.C., Kashemirov, B.A., McKenna, C.E. Ethylene Glycol-Linked Amino Acid Conjugates of Cyclic Cidofovir: Synthesis and Biological Activity, Nineteenth International Conference on Antiviral Research, San Juan, Puerto Rico. A58 (130) (2006).
Kim, J.S., Mitchell, S., Kijek, P., McKenna, C.E., Kashemirov, B.A., Eriksson, U., Breitenbach, J., Borysko, K., Amidon, G.L., Drach, J.C., Hilfinger, J.M. Stability, Transport, and Activity of Cidofovir Peptide Prodrugs, Nineteenth International Conference on Antiviral Research, San Juan, Puerto Rico. A58 (132) (2006).
Hilfinger, J.M., Wu, Z., Kim, J.S., Mitchell, S., Breitenbach, .J., Amidon, G.L, Drach, J.C. Vidarabine Prodrugs as Anti-Pox Virus Agents, Nineteenth International Conference on Antiviral Research, San Juan, Puerto Rico. A59 (138) (2006)
U. Eriksson, J.M. Hilfinger, J-S. Kim, S. Mitchell, P. Kijek, K.Z. Borysko, J.M. Breitenbach, J.C. Drach, B.A. Kashemirov, C.E. McKenna – Synthesis and biological activation of an ethylene glycol-linked amino acid conjugate of cyclic cidofovir. Bioorg Med Chem Lett. 2007 Feb 1;17(3):583-6 Epub (2006) Nov 10.
McKenna CE, Kashemirov BA, Eriksson U, Amidon GL, Kish PE, Mitchell S, Kim JS and Hilfinger JM. Cidofovir peptide conjugates as prodrugs. J. Organomet. Chem (2005) 690; 2673-2678
Song, X., P.L. Lorenzi, C.P. Landowski, B.S. Vig, J.M. Hilfinger, and G.L. Amidon, Amino acid ester prodrugs of the anticancer agent gemcitabine: synthesis, bioconversion, metabolic bioevasion, and hPEPT1-mediated transport. Mol Pharm, (2005). 2(2): p. 157-67.
Lorenzi, P.L., C.P. Landowski, X. Song, K.Z. Borysko, J.M. Breitenbach, J.S. Kim, J.M. Hilfinger, L.B. Townsend, J.C. Drach, and G.L. Amidon, Amino Acid Ester Prodrugs of 2-Bromo-5,6-dichloro-1-({beta}-D-ribofuranosyl) benzimidazole Enhance Metabolic Stability in Vitro and in Vivo. J Pharmacol Exp Ther, (2005). 314(2): p. 883-90.
S. Mittal, X. Song, B.S. Vig, C.P. Landowski, I. Kim, J.M. Hilfinger, and G.L. Amidon, Prolidase, a potential enzyme target for melanoma: design of proline-containing dipeptide-like prodrugs. Mol Pharm, (2005). 2(1): p. 37-46.
C.P. Landowski, X. Song, P.L. Lorenzi, J.M. Hilfinger, and G. L. Amidon, Floxuridine amino acid ester prodrugs: enhancing Caco-2 permeability and resistance to glycosidic bond metabolism. Pharm Res, (2005). 22(9): p. 1510-8.
Vig BS, Lorenzi PJ, Mittal S, Landowski CP, Shin HC, Mosberg HI, Hilfinger JM, Amidon GL. Amino acid ester prodrugs of floxuridine: synthesis and effects of structure, stereochemistry, and site of esterification on the rate of hydrolysis.Pharm Res. (2003) Sep;20(9):1381-8
Zimmermann EM, Schmiedlin-Ren L, Chamberlain J, Sabek M, Hilfinger JM, Parks E, Roessler BJ. Serotype 5 recombinant adenovirus selectively tranduces epithelial cells with a de-differentiated phenotype. American Gastroenterological Association, (2001).
Hsu C, Walter E, Merkle H, Rothen-Rutishauser B, Wunderli-Allenspach H, Hilfinger J, Amidon G. Function and immunolocalization of overexpressed human intestinal h+/peptide co-transporter in adenovirus-transduced caco-2 cells. AAPS PharmSci (1999);1 (3):E12
Hsu CP, Hilfinger JM, Walter E, Merkle HP, Roessler BJ, Amidon GL., Overexpression of human intestinal oligopeptide transporter in mammalian cells via adenoviral transduction. Pharmaceutical Research, 15(9):1376-81, (1998).
M.C.P. Hsu, J.M. Hilfinger and G.L. Amidon, Overexpression of human intestinal oligopeptide transporter in rat and human intestinal epithelial cell lines via adenoviral, Pharm.Res., 14, S-23 (Nov 1997) Boston, MA.
Ezra, A., Hoffman, A., Breuer, E., Weiss, G., Lipka, E., Amidon, G.L., Golomb, G.: Peptidyl prodrugs for improved oral absorption. Proceed. Intern. Symp. Control. Rel. Bioact. Mater. 24, p. 243 (1997)
Ezra, A., Breuer, E., Amidon, G.L., Hoffman, A., Ornoy, A., Patlas, N., Weiss, G., Lipka, E., Crison, J., Golomb, G.: Peptidyl prodrug of bisphosphonates for improved oral absorption. Proceed. Intern. Symp. Control. Rel. Bioact. Mater. 23, p. 83 (1996)
Ezra, A., Breuer, E., Amidon, G.L., Hoffman, A., Lipka, E., Weiss, G., Crison, J., Golomb, G.: Novel Bisphosphonates and Pepdidyl Prodrugs for Improved Oral Absorption. Pharm.Res. 13(9): S-358 (1996).
Lipka E, Crison JR, Amidon GL: Transmembrane Transport of Peptide Type Compounds: Prospect for Oral Delivery. J. Control. Rel. 39:121-129, (1996)
