Eprenetapopt

Eprenetapopt
Identifiers
	IUPAC name 2-(hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one;
CAS Number	5291-32-7;
PubChem CID	52918385;
DrugBank	DB11684;
ChemSpider	24606048;
UNII	Z41TGB4080;
KEGG	D12192;
ChEMBL	ChEMBL3186011;
CompTox Dashboard (EPA)	DTXSID401164013 ;
Chemical and physical data
Formula	C10H17NO3
Molar mass	199.250 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES COCC1(C(=O)C2CCN1CC2)CO;
	InChI InChI=1S/C10H17NO3/c1-14-7-10(6-12)9(13)8-2-4-11(10)5-3-8/h8,12H,2-7H2,1H3; Key:BGBNULCRKBVAKL-UHFFFAOYSA-N;

Eprenetapopt (APR-246) is an experimental anti-cancer drug which acts by reactivating certain mutant forms of p53, a tumour-suppressing gene which is commonly mutated into inactive forms as an early step in the development of malignant cancers. It has been researched over many years for treatment of numerous forms of cancer and reached late-stage clinical trials, but has never yet been approved for medical use due to inconsistent results. Nevertheless, it continues to be studied especially as a combination treatment alongside other anti-cancer medications, or in patients whose cancers have particular mutant forms of p53 thought to be susceptible to treatment with eprenetapopt.^[1]^[2]^[3]^[4]^[5]

References

^ Duffy MJ, Synnott NC, Crown J (September 2017). "Mutant p53 as a target for cancer treatment". European Journal of Cancer. 83: 258–265. doi:10.1016/j.ejca.2017.06.023. PMID 28756138.
^ Daver N, Wei AH, Pollyea DA, Fathi AT, Vyas P, DiNardo CD (October 2020). "New directions for emerging therapies in acute myeloid leukemia: the next chapter". Blood Cancer Journal. 10 (10): 107. doi:10.1038/s41408-020-00376-1. PMC 7599225. PMID 33127875.
^ Palacios-Berraquero ML, Alfonso-Piérola A (May 2021). "Current Therapy of the Patients with MDS: Walking towards Personalized Therapy". Journal of Clinical Medicine. 10 (10): 2107. doi:10.3390/jcm10102107. PMC 8153316. PMID 34068316.
^ Mishra A, Tamari R, DeZern AE, Byrne MT, Gooptu M, Chen YB, et al. (December 2022). "Eprenetapopt Plus Azacitidine After Allogeneic Hematopoietic Stem-Cell Transplantation for TP53-Mutant Acute Myeloid Leukemia and Myelodysplastic Syndromes". Journal of Clinical Oncology. 40 (34): 3985–3993. doi:10.1200/JCO.22.00181. PMID 35816664.
^ Pereira MP, Herrity E, Kim DD (April 2024). "TP53-mutated acute myeloid leukemia and myelodysplastic syndrome: biology, treatment challenges, and upcoming approaches". Annals of Hematology. 103 (4): 1049–1067. doi:10.1007/s00277-023-05462-5. PMID 37770618.

[1] Duffy MJ, Synnott NC, Crown J (September 2017). "Mutant p53 as a target for cancer treatment". European Journal of Cancer. 83: 258–265. doi:10.1016/j.ejca.2017.06.023. PMID 28756138.

[2] Daver N, Wei AH, Pollyea DA, Fathi AT, Vyas P, DiNardo CD (October 2020). "New directions for emerging therapies in acute myeloid leukemia: the next chapter". Blood Cancer Journal. 10 (10): 107. doi:10.1038/s41408-020-00376-1. PMC 7599225. PMID 33127875.

[3] Palacios-Berraquero ML, Alfonso-Piérola A (May 2021). "Current Therapy of the Patients with MDS: Walking towards Personalized Therapy". Journal of Clinical Medicine. 10 (10): 2107. doi:10.3390/jcm10102107. PMC 8153316. PMID 34068316.

[4] Mishra A, Tamari R, DeZern AE, Byrne MT, Gooptu M, Chen YB, et al. (December 2022). "Eprenetapopt Plus Azacitidine After Allogeneic Hematopoietic Stem-Cell Transplantation for TP53-Mutant Acute Myeloid Leukemia and Myelodysplastic Syndromes". Journal of Clinical Oncology. 40 (34): 3985–3993. doi:10.1200/JCO.22.00181. PMID 35816664.

[5] Pereira MP, Herrity E, Kim DD (April 2024). "TP53-mutated acute myeloid leukemia and myelodysplastic syndrome: biology, treatment challenges, and upcoming approaches". Annals of Hematology. 103 (4): 1049–1067. doi:10.1007/s00277-023-05462-5. PMID 37770618.

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