Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTQG4NR)

• DTT Name: Erythropoietin (EPO)
• Synonyms: Epoetin
• Gene Name: EPO
• DTT Type: Clinical trial target; [1]
• UniProt ID: EPO_HUMAN
• TTD ID: T07958
• Sequence:
  MGVHECPAWLWLLLSLLSLPLGLPVLGAPPRLICDSRVLERYLLEAKEAENITTGCAEHC
  SLNENITVPDTKVNFYAWKRMEVGQQAVEVWQGLALLSEAVLRGQALLVNSSQPWEPLQL
  HVDKAVSGLRSLTTLLRALGAQKEAISPPDAASAAPLRTITADTFRKLFRVYSNFLRGKL
  KLYTGEACRTGDR
• Function: Binds to EPOR leading to EPOR dimerization and JAK2 activation thereby activating specific downstream effectors, including STAT1 and STAT3. Hormone involved in the regulation of erythrocyte proliferation and differentiation and the maintenance of a physiological level of circulating erythrocyte mass.
• KEGG Pathway:
  Cytokine-cytokine receptor interaction (hsa04060)
  HIF-1 signaling pathway (hsa04066)
  PI3K-Akt signaling pathway (hsa04151)
  Jak-STAT signaling pathway (hsa04630)
  Hematopoietic cell lineage (hsa04640)
• Reactome Pathway: Regulation of gene expression by Hypoxia-inducible Factor (R-HSA-1234158)

Molecular Interaction Atlas (MIA) of This DTT

5 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LKA651	DMCFGP3	Diabetic macular edema	9B71.02	Phase 2	[2]
MK-2578	DM1M57I	Anemia	3A00-3A9Z	Phase 2	[1]
Erythropoietin-transfected autologous cell therapy	DMNZ6VA	Anemia	3A00-3A9Z	Phase 1/2	[3]
GC-1113	DMK96CE	Anemia	3A00-3A9Z	Phase 1	[4]
Long-acting erythropoietin conjugate	DM9OA35	Anemia	3A00-3A9Z	Phase 1	[5]

2 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
FC EPO	DMEX12T	Anemia	3A00-3A9Z	Discontinued in Phase 1	[6]
GLY-515n	DM0IKB4	Cerebrovascular ischaemia	8B1Z	Terminated	[7]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Shwachman-Diamond syndrome	3B64	Bone marrow	5.72E-01	-0.15	-0.83

References

• [1] Merck ditches biogeneric. Nat Biotechnol. 2010 Jul;28(7):636.
• [2] Clinical pipeline report, company report or official report of Novartis.
• [3] Mesenchymal stromal cells engineered to express erythropoietin induce anti-erythropoietin antibodies and anemia in allorecipients. Mol Ther. 2009 Feb;17(2):369-72.
• [4] A long-acting erythropoietin fused with noncytolytic human Fc for the treatment of anemia. Arch Pharm Res. 2012 May;35(5):757-9.
• [5] Company report (Pharmexcil)
• [6] Detection of EPO-Fc fusion protein in human blood: screening and confirmation protocols for sports drug testing. Drug Test Anal. 2012 Nov;4(11):818-29.
• [7] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027536)