190977-41-4

Basic information

• Product Name: OBLIMERSEN SODIUM
• Synonyms: OBLIMERSEN SODIUM;Augmerosen;Dna, D(p-thio)(T-C-T-C-C-C-A-G-C-G-T-G-C-G-C-C-A-T);Genasense;Unii-sh55B0rq9k
• CAS NO: 190977-41-4
• Molecular Formula: C172H204N62Na17O91P17S17
• Molecular Weight: 6058.305987
• Mol File: 190977-41-4.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• CAS DataBase Reference: OBLIMERSEN SODIUM(CAS DataBase Reference)
• NIST Chemistry Reference: OBLIMERSEN SODIUM(190977-41-4)
• EPA Substance Registry System: OBLIMERSEN SODIUM(190977-41-4)

Safety Data

• Hazardous Substances Data: 190977-41-4(Hazardous Substances Data)

Usage

Description

OBLIMERSEN SODIUM, also known as Genasense or G3139, is an 18-base phosphorothioate antisense oligodeoxynucleotide developed to treat various types of cancer, including chronic lymphocytic leukemia (CLL), B-cell lymphoma, lung, and breast cancers. It functions by binding to the first six codons of the Bcl-2 mRNA open reading frame, which leads to RNA cleavage by RNase H and downregulation of Bcl-2. This process results in both apoptotic and nonapoptotic antitumor effects.

Uses

Used in Pharmaceutical Industry:
OBLIMERSEN SODIUM is used as an antisense oligonucleotide for the treatment of cancer and rheumatological diseases. It works by downregulating the Bcl-2 protein, which is involved in preventing apoptosis (cell death) in cancer cells. This downregulation can lead to an increase in Bax and poly (ADP-ribose) Polymerase (PARP) to release cytochrome c and Smac/DIABLO, promoting apoptosis. Additionally, it may promote the release of Beclin-1 to induce autophagic cell death in the nonapoptotic pathway.
Furthermore, OBLIMERSEN SODIUM has been shown to enhance tumor immunity by promoting polyclonal antibody production and activating dendritic cell maturation. Although it failed in phase-III clinical trials as a monotherapy for lymphoid malignancies, it has been found to increase overall survival when combined with other chemotherapeutic drugs, such as dacarbazine, fludarabine, and cyclophosphamide, by increasing the sensitivity of these drugs.
Brand Name:
Genasense (Genta)

Clinical Use

Genta is developing a phosphorothioate antisense drug called oblimersen sodium that is complementary to the first six codons of the open reading frame of the human bcl-2 mRNA sequence. Oblimersen turns off production of the apoptosis inhibitor Bcl2 in tumor cells. This appears to increase a tumor cell's sensitivity to a variety of other anticancer therapies and, ultimately, may lead to cell death.