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. Author manuscript; available in PMC: 2019 Feb 4.
Published in final edited form as: Clin Genitourin Cancer. 2012 Oct 17;11(1):10–19. doi: 10.1016/j.clgc.2012.09.002

Figure 2.

Figure 2

B-Cell Lymphoma (Bcl-2) Inhibitors in Clinical and Preclinical Development for Genitourinary Cancers. There are Currently 2 Classes of Bcl-2 Inhibitors in Clinical and Preclinical Development for Genitourinary Cancers: (A) Antisense Oligonucleotides (ASO) and (B) Small Molecule BH3 Mimetics. The ASO, Oblimersen Sodium, (1) is in Phase ll/Phase III Clinical Trials in Prostate Cancer and Renal Cell Carcinoma and Specifically Hybridizes to the First 6 Codons of the Open Reading Frame of bcl-2 mRNA. (2) Oblimersen Promotes the Recruitment of Endogenous RNase H to Mediate bcl-2 mRNA Degradation, (3) Thereby Reducing Bcl-2 Protein Synthesis and Expression (4) and is Able to Recycle and Repeat the Process. (5) BH3 Mimetics Bind to the Hydrophobic BH3 Binding Domain of Specific Anti-Apoptotic Bcl-2 Family Members and Disrupt Their Ability to Oppose Apoptosis. BH3I-2 (Preclinical; Prostate Cancer) Targets Bcl-2. HA14–1 (Preclinical; Prostate Cancer) Targets Bcl-2. ABT-737 (Preclinical; Prostate Cancer, Renal Cell Carcinoma, Transitional Cell Carcinoma of Bladder) and Apogossypolone (Preclinical; Prostate Cancer) Target Bcl-xL, Bcl-2, and Bcl-w. AT-101 (Phase II; Prostate Cancer, Renal Cell Carcinoma, Transitional Cell Carcinoma of Bladder) and GX15–070 (not in Development in Genitourinary Cancers) Target Bcl-xL, Bcl-2, Bcl-w, and Mcl-1. Parenthesis Denotes Furthest Stage of Development for Genitourinary Cancers