生物活性：Mindeudesivir (JT001; VV116; GS-621763-d1) hydrobromide is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). Mindeudesivir hydrobromide retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19[1][2].
IC50 & Target：SARS-CoV-2, RSV[1][2]
体外研究(In Vitro)：氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱[1]。氘代化合物的潜在优势：
（1）延长体内半衰期。氘代化合物或能够延长化合物的药代动力学特征，即延长体内半衰期。由此可提高化合物安全性、有效性和耐受性，并增加给药的便捷性。
（2）提高口服生物利用度。氘代化合物或能够减少肠壁和肝脏中不需要的代谢 (首过代谢) 程度，使得更大比例的未代谢药物到达作用的目标位置。生物利用度高决定其在低剂量下具有活性以及更好的耐受性。
（3）改善代谢特征。氘代化合物或能够减少有毒或反应性代谢物的形成，改善药物代谢状况。
（4）改进药品安全性。氘代化合物或能够减少或消除药物化合物的不良副作用，具有安全性。
（5）保留治疗特性。氘代化合物有望保留和此前研究中氢类似物相似的生化效力和选择性。
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Mindeudesivir hydrobromide 相关抗体:
Acetyl CoA synthetase Antibody
Poliovirus Receptor Antibody (YA2556)
Cell Viability Assay
Cell Line:
A549 (infected with RSV)[1]
Concentration:
0-1000 μM
Incubation Time:
48 hours
Result:
Inhibited RSV replication in A549 cells with EC50 of 1.20 ± 0.32 μM, CC50 of 95.92 ± 9.27 μM and selectivity index (SI) of 80.
体内研究(In Vivo)
VV116 (25, 50 and 100 mg/kg; PO; b.i.d for 4 days) exhibits a stronger activity and decreases the virus titers below the detection limit at 50 mg/kg, also reduces lung injury after RSV infection[1].
VV116 (25, 50 and 100 mg/kg; PO; single dosage) exhibits favorable PK properties and good safety profile[1].
Pharmacokinetic Parameters of VV116 (JT001) in Balb/c mice[1].

PO (25 mg/kg)
PO (50 mg/kg)
PO (100 mg/kg)

Tmax (h)
0.42 ± 0.14
0.42 ± 0.14
0.42 ± 0.14
Cmax (ng/mL)
5360 ± 560
11617 ± 3443
24017 ± 6521
AUC0-t (ng/mL·h)
11461 ± 1013
24594 ± 1059
47799 ± 6545

AUC0-∞ (ng/mL·h)
11534 ± 992
24739 ± 1028
48014 ± 6696
MRT0-∞ (ng/mL·h)
2.25 ± 0.32
2.15 ± 0.26
2.28 ± 0.53
Tmax (h)
2.30 ± 1.10
3.27 ± 1.92
4.25 ± 0.53
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Balb/c mice[1]
Dosage:
25, 50 and 100 mg/kg
Administration:
PO; single dosage (Pharmacokinetics Analysis)
Result:
Exhibited favorable PK properties and good safety profile.
Animal Model:
Balb/c mice (6-8 weeks; intranasally infected with 4 × 10^6 FFU of RSV)[1]
Dosage:
25, 50 and 100 mg/kg
Administration:
PO; b.i.d for 4 days
Result:
Exhibited a stronger activity and decreased the virus titers below the detection limit at 50 mg/kg, also reduced lung injury after RSV infection.
Clinical Trial
NCT NumberSponsorConditionStart DatePhaseNCT05279235Shanghai Vinnerna Biosciences Co., Ltd.|Sponsor GmbHModerate to Severe COVID-19March 14, 2022Phase 3NCT05201690Vigonvita Life SciencesHealthy SubjectsDecember 14, 2021Phase 1NCT05227768Vigonvita Life SciencesHealthy SubjectsNovember 11, 2021Phase 1 NCT05242042Shanghai JunTop Biosciences Co., LTD|Sponsor GmbHMild to Moderate COVID-19January 28, 2022Phase 2|Phase 3NCT05355077Shanghai Vinnerna Biosciences Co., Ltd.Healthy SubjectsMay 2, 2022Phase 1NCT05221138Vigonvita Life SciencesHealthy SubjectsDecember 30, 2021Phase 1NCT05582629Shanghai Vinnerna Biosciences Co., Ltd.|Sponsor GmbHMild to Moderate COVID-19October 21, 2022Phase 3NCT05341609Vigonvita Life SciencesCOVID-19April 4, 2022Phase 3NCT05101135Jeil Pharmaceutical Co., Ltd.Type 2 Diabetes MellitusNovember 17, 2021Phase 3
分子量：583.45
Formula：C24H31DBrN5O7
CAS 号：2779498-79-0
性状：固体
颜色：White to light yellow
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)