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Synonyms: AZD-9150 | AZD9150 | ISIS STAT3Rx
Compound class:
Nucleic acid
Comment: Danvatirsen (AZD9150) is a phosphorothioate antisense oligonucleotide that was designed to inhibit expression of signal transducer and activator of transcription 3 (STAT3) as an anti-tumour mechanism [2-4]. It contains 2′-4′ constrained ethyl (cEt)-modified residues that increase affinity for target mRNA [2].
Full sequence as provided in the agent's INN record is: all-P-ambo-2'-O,4'-C-[(1S)-ethane-1,1-diyl]-5-methyl-P-thiocytidylyl-(3'→5')-2'-O,4'-C-[(1S)-ethane-1,1-diyl]-5-methyl-P-thiouridylyl-(3'→5')-2'-O,4'-C-[(1S)-ethane-1,1-diyl]-P-thioadenylyl-(3'→5')-P-thiothymidylyl-(3'→5')-P-thiothymidylyl-(3'→5')-P-thiothymidylyl-(3'→5')-2'-deoxy-P-thioguanylyl-(3'→5')-2'-deoxy-P-thioguanylyl-(3'→5')-2'-deoxy-P-thioadenylyl-(3'→5')-P-thiothymidylyl-(3'→5')-2'-deoxy-P-thioguanylyl-(3'→5')-P-thiothymidylyl-(3'→5')-2'-deoxy-5-methyl-P-thiocytidylyl-(3'→5')-2'-O,4'-C-[(1S)-ethane-1,1-diyl]-P-thioadenylyl-(3'→5')-2'-O,4'-C-[(1S)-ethane-1,1-diyl]-P-thioguanylyl-(3'→5')-2'-O,4'-C-[(1S)-ethane-1,1-diyl]-5-methylcytidine, but we have been unable to resolve this to a SMILES or HELM notation. |
| No information available. |
Summary of Clinical Use  |
| Danvatirsen is being investigated (in combination with other anti-tumour agents) for therapeutic efficacy in advanced cancers (e.g. NSCLC, HNSCC, AML/MDS) where standard-of-care treatments are ineffective. |
| Clinical Trials | |||||
| Clinical Trial ID | Title | Type | Source | Comment | References |
| NCT03334617 | Phase II Umbrella Study of Novel Anti-cancer Agents in Patients With NSCLC Who Progressed on an Anti-PD-1/PD-L1 Containing Therapy | Phase 2 Interventional | AstraZeneca | 1 | |
| NCT02983578 | Danvatirsen and Durvalumab in Treating Patients With Advanced and Refractory Pancreatic, Non-Small Cell Lung Cancer, and Mismatch Repair Deficient Colorectal Cancer | Phase 2 Interventional | M.D. Anderson Cancer Center | ||
| NCT05814666 | Activity and Safety of Danvatirsen and Pembrolizumab in HNSCC | Phase 2 Interventional | Flamingo Therapeutics NV | ||
| NCT05986240 | Danvatirsen Monotherapy Followed by Combination With Venetoclax in Relapsed/Refractory MDS & AML | Phase 1 Interventional | Montefiore Medical Center | ||
