Luxdegalutamide

Luxdegalutamide
Clinical data
Other names	ARV-766
Identifiers
	IUPAC name 4-[4-[[1-[4-[[3-(4-cyano-3-methoxyphenoxy)-2,2,4,4-tetramethylcyclobutyl]carbamoyl]phenyl]piperidin-4-yl]methyl]piperazin-1-yl]-N-[(3S)-2,6-dioxopiperidin-3-yl]-2-fluorobenzamide;
CAS Number	2750830-09-0;
PubChem CID	156504141;
ChemSpider	128921978;
UNII	5BD7R933PV;
ChEMBL	ChEMBL5314528;
Chemical and physical data
Formula	C45H54FN7O6
Molar mass	807.968 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1(C(C(C1OC2=CC(=C(C=C2)C#N)OC)(C)C)NC(=O)C3=CC=C(C=C3)N4CCC(CC4)CN5CCN(CC5)C6=CC(=C(C=C6)C(=O)N[C@H]7CCC(=O)NC7=O)F)C;
	InChI InChI=InChI=1S/C45H54FN7O6/c1-44(2)42(45(3,4)43(44)59-33-12-8-30(26-47)37(25-33)58-5)50-39(55)29-6-9-31(10-7-29)52-18-16-28(17-19-52)27-51-20-22-53(23-21-51)32-11-13-34(35(46)24-32)40(56)48-36-14-15-38(54)49-41(36)57/h6-13,24-25,28,36,42-43H,14-23,27H2,1-5H3,(H,48,56)(H,50,55)(H,49,54,57)/t36-,42?,43?/m0/s1; Key:RDPPBRKNBBXPNZ-PJXMSJPKSA-N;

Luxdegalutamide, also known as ARV-766, is an investigational oral androgen receptor (AR) degrader being developed by Arvinas for the treatment of metastatic castration-resistant prostate cancer (mCRPC).^[1]^[2] It belongs to a class of drugs called proteolysis targeting chimeras (PROTACs), which are designed to selectively degrade specific proteins by hijacking the ubiquitin-proteasome system.^[3] Luxdegalutamide is a second-generation PROTAC AR degrader that has demonstrated a broader efficacy profile and better tolerability compared to its predecessor, ARV-110, in clinical settings.^[3] It has shown promise in overcoming resistance associated with certain AR mutations, including the L702H mutation, which is prevalent in up to 24% of treated mCRPC patients.^[3] As of 2024, luxdegalutamide is being evaluated in phase I/II clinical trials for prostate cancer.^[1]^[2]

References

^ ^a ^b "Luxdegalutamide - Arvinas". AdisInsight. Springer Nature Switzerland AG.
^ ^a ^b Rej RK, Allu SR, Roy J, Acharyya RK, Kiran IN, Addepalli Y, et al. (April 2024). "Orally Bioavailable Proteolysis-Targeting Chimeras: An Innovative Approach in the Golden Era of Discovering Small-Molecule Cancer Drugs". Pharmaceuticals. 17 (4): 494. doi:10.3390/ph17040494. PMC 11054475. PMID 38675453.
^ ^a ^b ^c Israel JS, Marcelin LM, Thomas C, Szczyrbová E, Fuessel S, Puhr M, et al. (July 2024). "Emerging frontiers in androgen receptor research for prostate Cancer: insights from the 2nd international androgen receptor Symposium". Journal of Experimental & Clinical Cancer Research. 43 (1): 194. doi:10.1186/s13046-024-03125-5. PMC 11253403. PMID 39014480.

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[AdisInsight-1] "Luxdegalutamide - Arvinas". AdisInsight. Springer Nature Switzerland AG.

[Rej_2024-2] Rej RK, Allu SR, Roy J, Acharyya RK, Kiran IN, Addepalli Y, et al. (April 2024). "Orally Bioavailable Proteolysis-Targeting Chimeras: An Innovative Approach in the Golden Era of Discovering Small-Molecule Cancer Drugs". Pharmaceuticals. 17 (4): 494. doi:10.3390/ph17040494. PMC 11054475. PMID 38675453.

[Israel_2024-3] Israel JS, Marcelin LM, Thomas C, Szczyrbová E, Fuessel S, Puhr M, et al. (July 2024). "Emerging frontiers in androgen receptor research for prostate Cancer: insights from the 2nd international androgen receptor Symposium". Journal of Experimental & Clinical Cancer Research. 43 (1): 194. doi:10.1186/s13046-024-03125-5. PMC 11253403. PMID 39014480.

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