Voxelotor (GBT 440)

A modulator of sickle hemoglobin

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2mg

￥262.00

210.00

- +
5mg

￥537.00

430.00

- +
10mg

￥912.00

730.00

- +
50mg

￥2725.00

2180.00

- +
100mg

￥4850.00

3880.00

- +
400mg

￥13487.00

10790.00

- +

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Background

GBT-440 is a modulator of sickle hemoglobin (HbS) that binds covalently to the N-terminal valine of the α chain of HbS.¹ In vitro, GBT-440 increases HbS affinity for oxygen (EC₅₀s = 8.2 and 415 μM for purified HbS and whole blood from sickle cell anemia patients, respectively) and delays oxygen release from and polymerization of HbS in a concentration-dependent manner. GBT-440 (100-150 mg/kg) increases red blood cell half-life and reduces sickling ex vivo in whole blood isolated from a murine model of sickle cell anemia. It also reduces ex vivo sickling of sickle cell trait red blood cells under conditions of hypoxia, acidosis, and dehydration.²

1.Oksenberg, D., Dufu, K., Patel, M.P., et al.GBT440 increases haemoglobin oxygen affinity, reduces sickling and prolongs RBC half-life in a murine model of sickle cell diseaseBr. J. Haematol.175(1)141-153(2016) 2.Dufu, K., Lehrer-Graiwer, J., Ramos, E., et al.GBT440 inhibits sickling of sickle cell trait blood under in vitro conditions mimicking strenuous exerciseHematol. Rep.8(3)6637(2016)