Chemistry:Paltusotine

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Short description: Chemical compound

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Paltusotine
Paltusotine.svg
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC27H22F2N4O
Molar mass456.497 g·mol−1
3D model (JSmol)

Paltusotine is a selective somatostatin receptor type 2 (SST2) agonist in development for the treatment of acromegaly and certain neuroendocrine tumors. It is a small molecule delivered orally.[1][2][3][4]

References

  1. Madan, Ajay; Markison, Stacy; Betz, Stephen F.; Krasner, Alan; Luo, Rosa; Jochelson, Theresa; Lickliter, Jason; Struthers, R. Scott (April 2022). "Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers". Pituitary 25 (2): 328–339. doi:10.1007/s11102-021-01201-z. PMID 35000098. 
  2. Zhao, Jian; Wang, Shimiao; Markison, Stacy; Kim, Sun Hee; Han, Sangdon; Chen, Mi; Kusnetzow, Ana Karin; Rico-Bautista, Elizabeth et al. (12 January 2023). "Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist". ACS Medicinal Chemistry Letters 14 (1): 66–74. doi:10.1021/acsmedchemlett.2c00431. PMID 36655128. 
  3. Gadelha, Monica R; Gordon, Murray B; Doknic, Mirjana; Mezősi, Emese; Tóth, Miklós; Randeva, Harpal; Marmon, Tonya; Jochelson, Theresa et al. (13 April 2023). "ACROBAT Edge: Safety and Efficacy of Switching Injected SRLs to Oral Paltusotine in Patients With Acromegaly". The Journal of Clinical Endocrinology & Metabolism 108 (5): e148–e159. doi:10.1210/clinem/dgac643. PMID 36353760. 
  4. Zhao, Jie; Fu, Hong; Yu, Jingjing; Hong, Weiqi; Tian, Xiaowen; Qi, Jieyu; Sun, Suyue; Zhao, Chang et al. (21 February 2023). "Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine" (in en). Nature Communications 14 (1): 962. doi:10.1038/s41467-023-36673-z. ISSN 2041-1723. PMID 36810324. Bibcode2023NatCo..14..962Z.