cenersen

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cenersen

GtoPdb Ligand ID: 8270

Synonyms: Aezea® (proposed proprietary name) | EL625

Comment: Cenersen is a 20mer phosphorothioate antisense oligonucleotide complementary to a region of p53 messenger RNA [1]. The oligonucleotide sequence is reported as 5′-d[P-Thio](ccctgctccc ccctggctcc)-3′ [1]. This sequence matches nucleotides 1273-1292 of RefSeq nucleotide NM_000546 (Homo sapiens tumor protein p53 (TP53), transcript variant 1, mRNA).

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Summary of Clinical Use
Cenersen has been granted orphan drug designation by the EMA and FDA for the treament of chronic lymphocytic leukemia (CLL) and acute myeloid leukemia (AML). The FDA also includes treatment of stage IIB-IV melanoma in its orphan designation. Cenersen has not progressed beyond Phase 2 clinical trial, with 2 out of 3 trials being withdrawn or terminated early.

Summary of Clinical Use

Cenersen has been granted orphan drug designation by the EMA and FDA for the treament of chronic lymphocytic leukemia (CLL) and acute myeloid leukemia (AML). The FDA also includes treatment of stage IIB-IV melanoma in its orphan designation. Cenersen has not progressed beyond Phase 2 clinical trial, with 2 out of 3 trials being withdrawn or terminated early.

Mechanism Of Action and Pharmacodynamic Effects
In some types of cancer cells the p53 apoptitic pathway malfunctions, such that activated p53 acts as a pro-survival signal for tumourigenically damaged cells. Cenersen blocks the translation of wild type and mutant p53 proteins, so cells can undergo cell death via p53-independent mechanisms of apoptosis. It is expected that this may sensitize cancer cells to standard chemotherapy.

Mechanism Of Action and Pharmacodynamic Effects

In some types of cancer cells the p53 apoptitic pathway malfunctions, such that activated p53 acts as a pro-survival signal for tumourigenically damaged cells. Cenersen blocks the translation of wild type and mutant p53 proteins, so cells can undergo cell death via p53-independent mechanisms of apoptosis. It is expected that this may sensitize cancer cells to standard chemotherapy.