Details of the Drug Combination

General Information of Drug Combination (ID: DCBLD99)

• Drug Combination Name: Elacestrant + Alpelisib
• Indication: Breast Cancer; Status: Phase 1 [1]
• Component Drugs:
  Elacestrant (DM8RLJ5): N.A.
  Alpelisib (DMEXMYK): Small molecular drug

Molecular Interaction Atlas of This Drug Combination

Indication(s) of Elacestrant

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Approved	[2]

Elacestrant Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Estrogen receptor (ESR)	TTZAYWL	ESR1_HUMAN	Modulator	[5]

Indication(s) of Alpelisib

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Approved	[3]
Solid tumour/cancer	2A00-2F9Z	Phase 2	[4]

Alpelisib Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
PI3-kinase alpha (PIK3CA)	TTEUNMR	PK3CA_HUMAN	Inhibitor	[3]

Alpelisib Interacts with 1 DME Molecule(s)

DME Name	DME ID	UniProt ID	Mode of Action	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Metabolism	[6]

References

• [1] ClinicalTrials.gov (NCT05563220) Open-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Patients With Metastatic Breast Cancer
• [2] FDA Approved Drug Products from FDA Official Website. 2023. Application Number: 217639.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [4] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7955).
• [5] RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56.
• [6] Comparison of 19F NMR and 14C measurements for the assessment of ADME of BYL719 (Alpelisib) in humans. Drug Metab Dispos. 2017 Aug;45(8):900-907.