Hetrombopag

Hetrombopag
INN: Hetrombopag
Clinical data
Trade names	Hengqu
Other names	Rafutrombopag olamine; rafutrombopag ethanolamine; hetrombopag; SHR-8735; SHR8735
Routes of; administration	Oral
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name 5-[2-Hydroxy-3-[[5-methyl-3-oxo-2-(5,6,7,8-tetrahydronaphthalen-2-yl)-1H-pyrazol-4-yl]diazenyl]phenyl]furan-2-carboxylic acid;
CAS Number	2600513-51-5 ; 1257792-42-9 (rafutrombopag olamine);
PubChem CID	135565610;
IUPHAR/BPS	10657;
DrugBank	DB16184;
ChemSpider	52084807;
UNII	9WGT51BDDL;
ChEMBL	ChEMBL4594401;
Chemical and physical data
Formula	C25H22N4O5
Molar mass	458.474 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C(=O)N(N1)C2=CC3=C(CCCC3)C=C2)N=NC4=CC=CC(=C4O)C5=CC=C(O5)C(=O)O;
	InChI InChI=InChI=1S/C25H22N4O5/c1-14-22(24(31)29(28-14)17-10-9-15-5-2-3-6-16(15)13-17)27-26-19-8-4-7-18(23(19)30)20-11-12-21(34-20)25(32)33/h4,7-13,28,30H,2-3,5-6H2,1H3,(H,32,33); Key:YATJUTCKRWETAB-UHFFFAOYSA-N;

Hetrombopag (also known as rafutrombopag; trade name Hengqu) is a pharmaceutical drug for the treatment of thrombocytopenia and anemia.^[1]^[2]^[3]

It is a non-peptide small‐molecule thrombopoietin receptor agonist.^[4]

In China, it is approved for second-line treatment for primary immune thrombocytopenic purpura (ITP) and severe aplastic anemia (SAA) in adults.^[4]

References

^ Mei H, Chen X, Zhou J, Luo J, Shi Q, Liu J, et al. (January 2022). "Safety and efficacy of hetrombopag in patients with chronic immune thrombocytopenia: a single-arm, open-label, multi-center phase 1 study". Annals of Translational Medicine. 10 (2): 30. doi:10.21037/atm-21-4361. PMC 8848441. PMID 35282136.
^ Mei H, Liu X, Li Y, Zhou H, Feng Y, Gao G, et al. (February 2021). "A multicenter, randomized phase III trial of hetrombopag: a novel thrombopoietin receptor agonist for the treatment of immune thrombocytopenia". Journal of Hematology & Oncology. 14 (1): 37. doi:10.1186/s13045-021-01047-9. PMC 7905908. PMID 33632264.
^ Chang H, Pan L, Jia Y, Xiang B, Huang X, Guo Y, et al. (2023). "Effectiveness and Safety of Hetrombopag-Containing Therapy in Patients with Severe Aplastic Anemia: A Multicenter Real-World Study". Blood. 142: 5631. doi:10.1182/blood-2023-185469.
^ ^a ^b Syed YY (September 2021). "Hetrombopag: First Approval". Drugs. 81 (13): 1581–1585. doi:10.1007/s40265-021-01575-1. PMID 34357499.

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[1] Mei H, Chen X, Zhou J, Luo J, Shi Q, Liu J, et al. (January 2022). "Safety and efficacy of hetrombopag in patients with chronic immune thrombocytopenia: a single-arm, open-label, multi-center phase 1 study". Annals of Translational Medicine. 10 (2): 30. doi:10.21037/atm-21-4361. PMC 8848441. PMID 35282136.

[2] Mei H, Liu X, Li Y, Zhou H, Feng Y, Gao G, et al. (February 2021). "A multicenter, randomized phase III trial of hetrombopag: a novel thrombopoietin receptor agonist for the treatment of immune thrombocytopenia". Journal of Hematology & Oncology. 14 (1): 37. doi:10.1186/s13045-021-01047-9. PMC 7905908. PMID 33632264.

[3] Chang H, Pan L, Jia Y, Xiang B, Huang X, Guo Y, et al. (2023). "Effectiveness and Safety of Hetrombopag-Containing Therapy in Patients with Severe Aplastic Anemia: A Multicenter Real-World Study". Blood. 142: 5631. doi:10.1182/blood-2023-185469.

[Syed21-4] Syed YY (September 2021). "Hetrombopag: First Approval". Drugs. 81 (13): 1581–1585. doi:10.1007/s40265-021-01575-1. PMID 34357499.

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