ABTL0812
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| Other names | α-Hydroxylinoleic acid; 2-Hydroxylinoleic acid; ABTL-0812 |
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| Formula | C18H32O3 |
| Molar mass | 296.451 g·mol−1 |
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ABTL0812 (α-hydroxylinoleic acid) is a small-molecule, experimental cancer drug being developed by Ability Pharmaceuticals.[1]
History
[edit]In 2015, Ability announced that it had received orphan drug designation (ODD) for pediatric cancer neuroblastoma from the European Medical Agency (EMA) and the US Food and Drug Administration (FDA).[1] Also in 2016 a preclinical study confirmed that ABTL0812 was well tolerated.[2] In December 2016 the company announced ODD for the treatment of pancreatic cancer.[1]
Mechanism of action
[edit]One mechanism of action is the activation of the PPAR receptors and the TRIB3 gene, leading to inhibition of the Akt/mTOR pathway. This pathway is excessively activated in most human cancers, supporting tumor growth. It is a principal target of various new anti-tumour drugs. Tumor cells are killed viva autophagy, rather than apoptosis.[3][4]
ABTL0812 activates the PPAR receptors, inducing TRIB3 over-expression. TRIB3 binds to the Akt oncogene and inhibits the Akt/mTOR axis.[3]
Clinical trials
[edit]ABTL0812 showed efficacy in Phase I clinical trials in patients with advanced cancer, with low toxicity and high tolerability.[3]
References
[edit]- ^ a b c "Ability Pharmaceuticals Announces Orphan Drug Designation in the US for ABTL0812 in Pancreatic Cancer". Ability Pharmaceuticals SL.
- ^ "Ability Pharmaceuticals Announces Positive Phase 1 1b Study Results Of ABTL0812 In Cancer Patients With Advanced Solid Tumors". www.biospace.com.
- ^ a b c "New mechanism of antitumor action identified". Medical Xpress. 25 January 2016.
- ^ Erazo T, Lorente M, López-Plana A, Muñoz-Guardiola P, Fernández-Nogueira P, García-Martínez JA, et al. (May 2016). "The New Antitumor Drug ABTL0812 Inhibits the Akt/mTORC1 Axis by Upregulating Tribbles-3 Pseudokinase". Clinical Cancer Research. 22 (10): 2508–19. doi:10.1158/1078-0432.ccr-15-1808. hdl:2445/207600. PMID 26671995.