Oligonucleotide Pharmacology and Formulation: G3139 Anti-BCL2 Phosphorothioate In Stealth® Liposomes and Gel Implants

M. C. Woodle Genta Inc., 3550 General Atomics Ct., San Diego, CA, 92121

F. I. Raynaud The Institute of Cancer Research, Surrey, SM2 5NG, U.K.

M. Dizik Genta Inc., 3550 General Atomics Ct., San Diego, CA, 92121

O. Meyer University of California at San Francisco, San Francisco, CA, 94143

S. K. Huang SEQUUS Pharmaceuticals, Inc., 960 Hamilton Ct., Menlo Park, CA, 94025

J. A. Jaeger Genta Inc., 3550 General Atomics Ct., San Diego, CA, 92121

B. D. Brown Genta Inc., 3550 General Atomics Ct., San Diego, CA, 92121

R. Orr The Institute of Cancer Research, Surrey, SM2 5NG, U.K.

I. R. Judson The Institute of Cancer Research, Surrey, SM2 5NG, U.K.

D. Papahadjopoulos University of California at San Francisco, San Francisco, CA, 94143

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Abstract

G3139, an 18mer phosphorothioate, down regulates BCL2 and is efficacious in human xenograft tumor models. Studies of pharmacokinetics, toxicology, and influence of formulations on the biological properties of G3139 in mice are described. Bioavailability by s.c. and i.p. saline formulation injections are similar, about 60%.

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Oligonucleotide Pharmacology and Formulation: G3139 Anti-BCL2 Phosphorothioate In Stealth® Liposomes and Gel Implants

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Oligonucleotide Pharmacology and Formulation: G3139 Anti-BCL2 Phosphorothioate In Stealth® Liposomes and Gel Implants

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