MK-2206

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MK-2206
MK-2206.svg
Names
IUPAC name
8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one
Identifiers
3D model (JSmol)
ChemSpider
ECHA InfoCard 100.207.435
Properties
C25H21N5O
Molar mass 407.477 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

MK-2206 is a drug candidate being investigated to help treat cancer. Its chemical formula is C25H21N5O.[1] It acts as an allosteric AKT inhibitor.[2]

It is a highly selective inhibitor of pan-Akt, namely, of all three Akt isoforms Akt1, Akt2, and Akt3.[1]

It is intended to be used with other cancer therapies that advanced tumours may become resistant to.[3]

Clinical trials[edit]

2011: A phase 1 clinical trial of MK-2206 alone has reported it was well tolerated.[4]
2014: A phase 1 clinical trial of MK-2206 with a variety of other agents in 72 patients with advanced cancer reported acceptable side-effects.[3]
2016: MK-2206 is one of the treatments in the I-SPY2 Adaptive clinical trial for breast cancer that had been selected for later stage trials.[5]
As of August 2017 31 phase II clinical trials are registered, many completed.[6] e.g. in colorectal cancer, breast cancer, and many others.

References[edit]

  1. ^ a b MK-2206 dihydrochloride (CAS 1032350-13-2) inc structure diagram
  2. ^ MK-2206, an Allosteric Akt Inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular Targeted Drugs In vitro and In vivo. Hirai et al. 2010
  3. ^ a b A trial of MK-2206 with chemotherapy or erlotinib for advanced cancer
  4. ^ Yap, TA; Yan, L; Patnaik, A; Fearen, I; Olmos, D; Papadopoulos, K; Baird, RD; Delgado, L; Taylor, A; Lupinacci, L; Riisnaes, R; Pope, LL; Heaton, SP; Thomas, G; Garrett, MD; Sullivan, DM; de Bono, JS; Tolcher, AW (2011). "First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors". J Clin Oncol. 29: 4688–95. doi:10.1200/JCO.2011.35.5263. PMID 22025163.
  5. ^ Novel Agents are Targeting Drivers of TNBC - Several drug candidates in I-SPY2 have 'graduated' to later-phase studies. June 2016
  6. ^ MK-2206 phase=2 trials