Adavosertib

Adavosertib (development codes AZD1775, MK-1775) is an experimental anti-cancer drug candidate. It is a small molecule inhibitor of the tyrosine kinase WEE1 with potential antineoplastic sensitizing activity.[1] It is being developed by AstraZeneca.[2] It is being investigated as a treatment for pancreatic cancer with a phase 1 trial (University of Michigan researchers are as of 2019 planning a phase 2 study.[3]), and ovarian cancer, in combination with another anti-cancer drug, gemcitabine, as a phase 2 trial.[4][5][6]

Adavosertib
Names
Preferred IUPAC name
1-[6-(2-Hydroxypropan-2-yl)pyridin-2-yl]-6-[4-(4-methylpiperazin-1-yl)anilino]-2-(prop-2-en-1-yl)-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one
Other names
AZD1775; MK-1775
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
ECHA InfoCard 100.205.373
KEGG
UNII
  • InChI=1S/C27H32N8O2/c1-5-13-34-25(36)21-18-28-26(29-19-9-11-20(12-10-19)33-16-14-32(4)15-17-33)31-24(21)35(34)23-8-6-7-22(30-23)27(2,3)37/h5-12,18,37H,1,13-17H2,2-4H3,(H,28,29,31)
    Key: BKWJAKQVGHWELA-UHFFFAOYSA-N
  • CN1CCN(CC1)c2ccc(Nc3ncc4C(=O)N(CC=C)N(c5cccc(n5)C(C)(C)O)c4n3)cc2
Properties
C27H32N8O2
Molar mass 500.607 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

References
  1. "NCI Drug Dictionary". National Cancer Institute. 2 February 2011. Retrieved 17 August 2019.
  2. "AZD1775 | AstraZeneca Open Innovation". openinnovation.astrazeneca.com. Archived from the original on 17 August 2019. Retrieved 17 August 2019.
  3. "AstraZeneca drug heads to phase 2 in pancreatic cancer after small trial extends survival". FierceBiotech. Retrieved 17 August 2019.
  4. Lheureux, Stephanie; Cristea, Mihaela C.; Bruce, Jeffrey P.; Garg, Swati; Cabanero, Michael; Mantia-Smaldone, Gina; Olawaiye, Alexander B.; Ellard, Susan L.; Weberpals, Johanne I.; Wahner Hendrickson, Andrea E.; Fleming, Gini F.; Welch, Stephen; Dhani, Neesha C.; Stockley, Tracy; Rath, Prisni (2021-01-23). "Adavosertib plus gemcitabine for platinum-resistant or platinum-refractory recurrent ovarian cancer: a double-blind, randomised, placebo-controlled, phase 2 trial". Lancet. 397 (10271): 281–292. doi:10.1016/S0140-6736(20)32554-X. ISSN 1474-547X. PMID 33485453. S2CID 231667519.
  5. "Early Activity in Pancreatic Cancer With New Drug". www.medpagetoday.com. 16 August 2019. Retrieved 17 August 2019.
  6. Cuneo KC, Morgan MA, Sahai V, Schipper MJ, Parsels LA, Parsels JD, et al. (October 2019). "Dose Escalation Trial of the Wee1 Inhibitor Adavosertib (AZD1775) in Combination With Gemcitabine and Radiation for Patients With Locally Advanced Pancreatic Cancer". Journal of Clinical Oncology. 37 (29): 2643–2650. doi:10.1200/JCO.19.00730. PMC 7006846. PMID 31398082.


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