Drug intelligence / Profile preview

oblimersen + fludarabine + rituximab

Development stage
Unknown
Lead developer
Genta
Modality
Small Molecules, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

rejuvenates **Oblimersen + fludarabine + rituximab** is a three-drug combination regimen investigated for the treatment of relapsed or refractory chronic lymphocytic leukemia (CLL) and other lymphoid malignancies. Oblimersen is an antisense oligonucleotide targeting Bcl-2 mRNA, thereby reducing Bcl-2 protein expression and promoting apoptosis in malignant cells. Fludarabine is a purine analog acting as a cytotoxic small molecule by inhibiting DNA polymerase and ribonucleotide reductase, leading to termination of DNA synthesis. Rituximab is a monoclonal antibody against CD20, a B-cell surface antigen, which induces cell death via complement-dependent cytotoxicity, antibody-dependent cellular cytotoxicity, and direct apoptosis. Preclinical and clinical studies suggest that oblimersen may enhance the apoptotic effects of fludarabine and rituximab, resulting in increased response rates and molecular remissions in patients with CLL[1][5][7].

Brand names
GenasenseRituxan
Other names
oblimersen sodium
02

Targets

DNA polymerase familyBCL-2 (BCL-2 family)CD20 (B-lymphocyte antigen CD20)RNR (Ribonucleotide reductase)

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