Table 4 Clinical application of BH3-mimetics targeting anti-apoptotic Bcl-2 family proteins. (clinicaltrials.gov)

Bcl-xL

A-1155463

Structure-based design.

Preclinical

[159]

A-1331852

Structure-based design.

Preclinical

[160]

WEHI-539

Structure- based design

Preclinical

[161]

DT2216

Proteolysis targeting chimera

Preclinical

[162]

XZ424

Proteolysis targeting chimera

Preclinical

[163]

ABBV-155

Structure-based design

Phase I

NCT03595059

Bcl-xL

Bcl-2

AZD4320

Structure-based design

Preclinical

[164]

BM-957

Structure-based design

Preclinical

[165]

BM-1197

Structure-based design

Preclinical

[166]

S44563

Structure-based design

Preclinical

[167]

APG-1252

Structure-based design

Phase I/II

[168]

Bcl-xL

Bcl-2

Bcl-w

Ch282-5

Gossypol derivative

Preclinical

[169]

ABT-737

Synthetic, acylsulfonamide-based

Phase I/II

[170]

ABT-263 (Navitoclax)

Derivant of ABT-737

Phase I/II/III

[171]

Bcl-xL, Bcl-2, Mcl-1

BH3-M6

Synthetic terphenyl scaffold

Preclinical

[172]

Bcl-xL, Bcl-2,

Bcl-w, Mcl-1

TW-37

Benzenesulfonyl derivative of gossypol

Preclinical

[173]

BI-97C1 (Sabutoclax)

Diastereoisomer of Apogossypol

Preclinical

[174]

BIM-SAHB

Stapled Bim peptide

Preclinical

[175]

GX15-070 (Obatoclax)

Synthetic indolyl-dipyrromethene

Phase I/II/III

[176]

AT-101

(−)-gossypol enantiomer

Phase I/II/III

[177]

Bcl-2

S55746

Structure-based design

Phase I

[178]

ABT-199 (Venetoclax)

Derivant of ABT-263

Phase I/II/III

[127]

Mcl-1

A-1210477

Structure-based design

Preclinical

[179]

UMI-77

Structure-based design

Preclinical

[180]

VU661013

Fragment-based lead generation

Preclinical

[181]

S63845

Structure-based design

Preclinical

[182]

AMG176,

Structure-based design

Phase I

[183]

AZD5991

Structure-based design

Phase I

[184]

S64315

Fragment-based lead generation

Phase I/II

[182]

Bcl-2, Mcl-1

S1-6

Structure-based design

Preclinical

[185]

Nap-1

Derivant of S1-6

Preclinical

[186]