Thursday, December 15, 2016

CPLA2 (Cytosolic Phospholipase A2) Inhibitor AK106-001616

I had been interested in the CPLA2 (cytosolic phospholipase A2) inhibitor AK106-001616, when a study had been presented at the 2013 EULAR Annual Meeting. This year (2016) didn’t see any study being presented at the EULAR or ACR Annual Meetings. CPLA2 inhibition would also inhibit the downstream enzyme COX-2.

Last year there had been a study by T. Kozaki and colleagues, who looked of drug-drug interaction between the AK106-001616 and methotrexate in rheumatoid arthritis patients. The authors found a weak drug interaction between AK106-001616 and MTX, which is due to an altered MTX transport in renal proximal tubules.

K. Ohuchi and colleagues published a study on the protective effect of AK106-001616 on induced cell death in a murine motor neuron-like cell.
The NHS Health Research Authority reports a study in 2011: “A Phase IIa, Multi-Centre, Randomised, Double-Blind, Comparator Controlled, Repeated-Dose Study of 2 Dose Levels of AK106 001616 in Patients with Rheumatoid Arthritis”.

AdisInsight reports a phase 2 study for rheumatoid arthritis ongoing in Europe for 2015.

“To sum it up, I don’t see an important role of AK 106 in the treatment of RA patients.” Still!


Kozaki T, Tagashira M, Yamanishi K, Ellis B, Kayanoki T, Ooishi R, Sugiyama K, Matsuda S, Tsuruta K, Kohira T, Tsurui K.: Evaluation of drug-drug interaction between the novel cPLA2 inhibitor AK106-001616 and methotrexate in rheumatoid arthritis patients. Xenobiotica. 2015;45(7):615-24. doi: 10.3109/00498254.2014.1000430. Epub 2015 Jan 12.

Ohuchi, K. , Tsuruma, K. , Shimazawa, M. , Nakamura, J. and Hara, H. (2016) The Novel cPLA2 Inhibitor AK106-001616 Has a Protective Effect on SOD1G93A-Induced Cell Death in NSC34 Murine Motor Neuron-Like Cell. Pharmacology & Pharmacy, 7, 193-199. doi: 10.4236/pp.2016.75025.

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