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. 2021 Aug 2;289(20):6209–6234. doi: 10.1111/febs.16136

Table 3.

Summary of MCL1 inhibitors under clinical trials.

Compound, chemical structure, and institution Potency (TR‐FRET) Clinical trials a Study Administration Indication References

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AZD5991

AstraZeneca

MCL1 K i = 0.2 nm

BCL2 K i = 6.8 μm

BCL‐xL K i = 18 μm

BCLW K i = 25 μm

BFL1 K i = 12 μm

NCT03218683 Phase I, monotherapy, and combination IV Refractory Hematological malignancies [213]

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AMG‐176

Amgen

MCL1 K i = 0.06 nm

BCL2 K i = 0.95 μm

BCL‐xL K i = 0.7 μm

NCT02675452 Phase I, monotherapy IV Relapsed or refractory MM/AML [159]
NCT03797261 Phase I, monotherapy with venetoclax IV AML/Lymphoma

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AMG‐397

Amgen

Not disclosed NCT03465540 Phase I, monotherapy Oral MM/AML/NHL [214]

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S64315/MIK665

Servier/Novartis

MCL1 K i = 1.2 nm NCT02979366 Phase I, monotherapy IV AML/MDS [156]
NCT02992483 Phase I, monotherapy IV MM/Lymphoma
NCT03672695 Phase I, combination with venetoclax IV AML/MDS
NCT04629443 Phase II, combination with azacitidine IV AML
NCT04702425 Phase I, combination with VOB560 IV NHL/AML/MM

Structure not disclosed

ABBV‐467

AbbVie

Not disclosed NCT04178902 Phase I, monotherapy IV MM Not disclosed

Structure not disclosed

PRT1419

Prelude Therapeutics

Not disclosed NCT04543305 Phase I, monotherapy Oral Refractory Hematological malignancies Not disclosed
NCT04837677 Phase I, monotherapy IV Relapsed or refractory solid tumors