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US Approved Rx

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Primary Target

Cyclin-dependent kinase 4

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Cyclin-dependent kinase 6

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IMR-5

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SH-SY5Y

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(HER2)-negative advanced or metastatic breast cancer

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Breast cancer

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Astex Therapeutics

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Protein kinase inhibitors

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Showing 1 - 6 of 6 results

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RIBOCICLIB

TK8ERE8P56

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Status:

US Approved Rx (2017)

First approved in 2017

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Cyclin-dependent kinase 4

Cyclin-dependent kinase 6

Conditions:

(HER2)-negative advanced or metastatic breast cancer

Ribociclib, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK...

4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. Ribociclib is in phase III clinical trials by Novartis for the treatment of postmenopausal women with advanced breast cancer. Phase II clinical trials are also in development for the treatment of liposarcoma, ovarian cancer, fallopian tube cancer, peritoneum cancer, endometrial cancer, and gastrointestinal cancer. Preregistration for Breast cancer (First-line therapy, Combination therapy, Late-stage disease) in the USA (PO) in November 2016.

BENZOPHENONE IMINE

EJJ21NA7VI

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

ISOBUTYL BROMIDE

5OEC0BW987

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

RIBOCICLIB HYDROCHLORIDE

63YF7YKW7E

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Status:

US Approved Rx (2017)

First approved in 2017

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Cyclin-dependent kinase 4

Cyclin-dependent kinase 6

Conditions:

(HER2)-negative advanced or metastatic breast cancer

Ribociclib, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK...

4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. Ribociclib is in phase III clinical trials by Novartis for the treatment of postmenopausal women with advanced breast cancer. Phase II clinical trials are also in development for the treatment of liposarcoma, ovarian cancer, fallopian tube cancer, peritoneum cancer, endometrial cancer, and gastrointestinal cancer. Preregistration for Breast cancer (First-line therapy, Combination therapy, Late-stage disease) in the USA (PO) in November 2016.

RIBOCICLIB SUCCINATE

BG7HLX2919

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Status:

US Approved Rx (2017)

First approved in 2017

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Cyclin-dependent kinase 4

Cyclin-dependent kinase 6

Conditions:

(HER2)-negative advanced or metastatic breast cancer

Ribociclib, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK...

4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. Ribociclib is in phase III clinical trials by Novartis for the treatment of postmenopausal women with advanced breast cancer. Phase II clinical trials are also in development for the treatment of liposarcoma, ovarian cancer, fallopian tube cancer, peritoneum cancer, endometrial cancer, and gastrointestinal cancer. Preregistration for Breast cancer (First-line therapy, Combination therapy, Late-stage disease) in the USA (PO) in November 2016.

BENZOPHENONE IMINE HYDROCHLORIDE

M8RM3S474H

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

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