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Development Status

Investigational

2

Other

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Primary Target

Bromodomain-containing protein 2

2

Bromodomain-containing protein 3

2

Bromodomain-containing protein 4

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Highest Phase

Phase II

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Approval Year

Unknown

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Condition

Castrate-resistant prostate cancer

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Glioblastoma multiforme

2

Hematologic malignancies

2

Non-small cell lung cancer

2

Pancreatic ductal adenocarcinoma

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Treatment Modality

Primary

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CNS Activity

CNS Penetrant

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Originator

Mitsubishi Tanabe Pharma

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Substance Class

Chemical

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Code System

CAS

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FDA UNII

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PUBCHEM

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EPA CompTox

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WIKIPEDIA

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Substance Form

Principal Form

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Salts, Hydrates, Esters, etc.

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Showing 1 - 4 of 4 results

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BIRABRESIB

X40LKS49S3

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Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Bromodomain-containing protein 4

Bromodomain-containing protein 3

Bromodomain-containing protein 2

Conditions:

Castrate-resistant prostate cancer

Pancreatic ductal adenocarcinoma

Hematologic malignancies

Glioblastoma multiforme

Triple-negative breast cancer

Non-small cell lung cancer

The BET-bromodomain inhibitor OTX015 (MK-8628) was initially developed by Mitsubishi Tanabe Pharma Corporation, but then was licensed by OncoEthix, privately held biotechnology company. OTX015 is a selective bromodomains: BRD2, BRD3, and BRD4 inhibi...

tor and inhibits their binding to AcH4. Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and differentiation to energy homeostasis and neurological processes. OTX015 has potent antiproliferative activity accompanied by c-MYC down-regulation in several tumor types, and has demonstrated synergism with the mTOR inhibitor everolimus in different models. Oral administration of OTX-015 markedly inhibited tumor growth and reduced tumor volume. OTX015 is currently in Phase 1b studies for the treatment of hematological malignancies and advanced solid tumors such as Triple Negative Breast Cancer, Non-small Cell Lung Cancer, Castrate-resistant Prostate Cancer (CRPC) and Pancreatic Ductal Adenocarcinoma. In addition, OTX015 was in phase II for the treatment of Glioblastoma Multiforme, but there were not detected clinical activity of the drug in the treatment populations and trial was closed.

PIVALOYL CHLORIDE

JQ82J0O21T

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

ETHYL CARBONATE

3UA92692HG

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

BIRABRESIB DIHYDRATE

4Q356KA5V2

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Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Bromodomain-containing protein 4

Bromodomain-containing protein 3

Bromodomain-containing protein 2

Conditions:

Castrate-resistant prostate cancer

Pancreatic ductal adenocarcinoma

Hematologic malignancies

Glioblastoma multiforme

Triple-negative breast cancer

Non-small cell lung cancer

The BET-bromodomain inhibitor OTX015 (MK-8628) was initially developed by Mitsubishi Tanabe Pharma Corporation, but then was licensed by OncoEthix, privately held biotechnology company. OTX015 is a selective bromodomains: BRD2, BRD3, and BRD4 inhibi...

tor and inhibits their binding to AcH4. Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and differentiation to energy homeostasis and neurological processes. OTX015 has potent antiproliferative activity accompanied by c-MYC down-regulation in several tumor types, and has demonstrated synergism with the mTOR inhibitor everolimus in different models. Oral administration of OTX-015 markedly inhibited tumor growth and reduced tumor volume. OTX015 is currently in Phase 1b studies for the treatment of hematological malignancies and advanced solid tumors such as Triple Negative Breast Cancer, Non-small Cell Lung Cancer, Castrate-resistant Prostate Cancer (CRPC) and Pancreatic Ductal Adenocarcinoma. In addition, OTX015 was in phase II for the treatment of Glioblastoma Multiforme, but there were not detected clinical activity of the drug in the treatment populations and trial was closed.

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