Chemistry:Avadomide

From HandWiki

Avadomide (CC-122) is an experimental cereblon E3 ligase modulator, or thalidomide analog (molecular glue) that was discovered and studied by Celgene to see if it was effective against cancer.[1][2][3][4][5] The deuterated S-enantiomer, SP-3164 (DRX-164) is in development at Salarius Pharmaceuticals.[6][7]

References

  1. ↑ Nishi, Hidemi; Gotoh, Kunihito; Tomimaru, Yoshito; Kobayashi, Shogo; Sasaki, Kazuki; Iwagami, Yoshifumi; Yamada, Daisaku; Akita, Hirofumi et al. (October 2023). "Anti-tumor effect of avadomide in gemcitabine-resistant pancreatic ductal adenocarcinoma". Cancer Chemotherapy and Pharmacology 92 (4): 303–314. doi:10.1007/s00280-023-04531-w. PMID 37491611. 
  2. ↑ Nastoupil, Loretta J.; Kuruvilla, John; Chavez, Julio C.; Bijou, Fontanet; Witzig, Thomas E.; Santoro, Armando; Flinn, Ian W.; Boccomini, Carola et al. (May 2022). "Phase Ib study of avadomide (CC-122) in combination with rituximab in patients with relapsed/refractory diffuse large B-cell lymphoma and follicular lymphoma". EJHaem 3 (2): 394–405. doi:10.1002/jha2.394. PMID 35846031. 
  3. ↑ Heim, Christopher; Hartmann, Marcus D. (1 March 2022). "High-resolution structures of the bound effectors avadomide (CC-122) and iberdomide (CC-220) highlight advantages and limitations of the MsCI4 soaking system". Acta Crystallographica Section D Structural Biology 78 (3): 290–298. doi:10.1107/S2059798322000092. PMID 35234143. Bibcode: 2022AcCrD..78..290H. 
  4. ↑ Hagner, Patrick R.; Chiu, Hsiling; Chopra, Vivek S.; Colombo, Martino; Patel, Nisha; Estevez, Maria Ortiz; Waldman, Michelle F.; Loos, Remco et al. (2 August 2022). "Interactome of Aiolos/Ikaros Reveals Combination Rationale of Cereblon Modulators with HDAC Inhibitors in DLBCL". Clinical Cancer Research 28 (15): 3367–3377. doi:10.1158/1078-0432.CCR-21-3347. PMID 35583604. 
  5. ↑ Ribrag, Vincent; Chavez, Julio C.; Boccomini, Carola; Kaplan, Jason; Chandler, Jason C.; Santoro, Armando; Corradini, Paolo; Flinn, Ian W. et al. (February 2022). "Phase Ib study of combinations of avadomide (CC-122), CC-223, CC-292, and rituximab in patients with relapsed/refractory diffuse large B-cell lymphoma". EJHaem 3 (1): 139–153. doi:10.1002/jha2.375. PMID 35846221. 
  6. ↑ Jacques, Vincent; Czarnik, Anthony W; Judge, Thomas M; Van der Ploeg, Lex HT; DeWitt, Sheila (2015). "Differentiation of antiinflammatory and antitumorigenic properties of stabilized enantiomers of thalidomide analogs". Proc Natl Acad Sci U S A 112 (12): E1471. doi:10.1073/pnas.1417832112. PMID 25775521. 
  7. ↑ Santiesteban, Daniela Y; Duncan, Aundrietta D; Mirza, Nadeem Q; Jacques, Vincent; DeWitt, Sheila; Iyer, Swami P. (15 November 2022). "SP-3164, a Novel Cereblon-Binding Protein Degrader, Shows Activity in Preclinical Lymphoma Models". Blood 140 (Supplement 1): 8865–8866. doi:10.1182/blood-2022-167495. 



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