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Primary Target

Histone deacetylase 7

4

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

237

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US Approved Rx

3

Investigational

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Phase III

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Approval Year

2024

3

Unknown

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Duchenne muscular dystrophy

3

Polycythemia vera

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Systemic onset juvenile idiopathic arthritis

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Advanced solid cancer

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Primary

4

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CNS Penetrant

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Italfarmaco

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Novartis

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EPA CompTox

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Showing 1 - 4 of 4 results

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Givinostat

5P60F84FBH

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Status:

US Approved Rx (2024)

First approved in 2024

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Histone deacetylase 2

Histone deacetylase 3

Histone deacetylase 6

Histone deacetylase 7

Histone deacetylase 1

Histone deacetylase 4

Conditions:

Systemic onset juvenile idiopathic arthritis

Polycythemia vera

Duchenne muscular dystrophy

Gavinostat is an orally bioavailable hydroxymate inhibitor of histone deacetylase (HDAC) with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. Gavinostat inhibits class I and class II HDACs, resulting in an accumulation of...

highly acetylated histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression. At low, nonapoptotic concentrations, this agent inhibits the production of pro-inflammatory cytokines such as tumor necrosis factor- (TNF-), interleukin-1 (IL-1), IL-6 and interferon-gamma. It is currently in phase 2 trials for Myeloproliferative disorders, Polycythaemia vera and Phase III for Duchenne muscular dystrophy announced. In clinical trials of givinostat as a salvage therapy for advanced Hodgkin's lymphoma, the most common adverse reactions were fatigue, mild diarrhea or abdominal pain, moderate thrombocytopenia, and mild leukopenia.

DACINOSTAT

V10P524501

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Histone deacetylase 11

Histone deacetylase 3

Histone deacetylase 10

Histone deacetylase

Histone deacetylase 1

Histone deacetylase 2

Histone deacetylase 6

Histone deacetylase 9

Histone deacetylase 8

Histone deacetylase 7

Histone deacetylase 5

Histone deacetylase 4

Conditions:

Advanced solid cancer

Dacinostat (also known as LAQ824), is a hydroxamate histone deacetylase inhibitor with potential anticancer activity. Dacinostat inhibits histone deacetylase enzymatic activities in vitro and transcriptionally activated the p21 promoter in reporter g...

ene assays. Tumor cells treated with Dacinostat caused acetylation of HSP90 and degradation of its cargo oncoproteins. Flow cytometry studies revealed that both tumor cell lines and normal diploid fibroblasts arrested in the G2/M phase of the cell cycle after Dacinostat treatment. However, an increased sub-G1 population at 48 h (reminiscent of apoptotic cells) was only observed in the cancer cell lines treated with Dacinostat. Dacinostat exhibited antitumor effects in a xenograft animal models. In phase I trials, Dacinostat was well tolerated at doses that induced accumulation of histone acetylation, with higher doses inducing changes consistent with HSP90 inhibition. In another phase 1 in patients with advanced solid tumors, grade 3 or 4 toxicities were observed. Dacinostat had been in phase II clinical trials by Novartis for the treatment of solid tumors but further studies were discontinued.

Givinostat Hydrochloride

6R2GQ94CB5

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Status:

US Approved Rx (2024)

First approved in 2024

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Histone deacetylase 2

Histone deacetylase 3

Histone deacetylase 6

Histone deacetylase 7

Histone deacetylase 1

Histone deacetylase 4

Conditions:

Systemic onset juvenile idiopathic arthritis

Polycythemia vera

Duchenne muscular dystrophy

Gavinostat is an orally bioavailable hydroxymate inhibitor of histone deacetylase (HDAC) with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. Gavinostat inhibits class I and class II HDACs, resulting in an accumulation of...

highly acetylated histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression. At low, nonapoptotic concentrations, this agent inhibits the production of pro-inflammatory cytokines such as tumor necrosis factor- (TNF-), interleukin-1 (IL-1), IL-6 and interferon-gamma. It is currently in phase 2 trials for Myeloproliferative disorders, Polycythaemia vera and Phase III for Duchenne muscular dystrophy announced. In clinical trials of givinostat as a salvage therapy for advanced Hodgkin's lymphoma, the most common adverse reactions were fatigue, mild diarrhea or abdominal pain, moderate thrombocytopenia, and mild leukopenia.

Givinostat hydrochloride anhydrous

Z02132R2QQ

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Status:

US Approved Rx (2024)

First approved in 2024

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Histone deacetylase 2

Histone deacetylase 3

Histone deacetylase 6

Histone deacetylase 7

Histone deacetylase 1

Histone deacetylase 4

Conditions:

Systemic onset juvenile idiopathic arthritis

Polycythemia vera

Duchenne muscular dystrophy

Gavinostat is an orally bioavailable hydroxymate inhibitor of histone deacetylase (HDAC) with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. Gavinostat inhibits class I and class II HDACs, resulting in an accumulation of...

highly acetylated histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression. At low, nonapoptotic concentrations, this agent inhibits the production of pro-inflammatory cytokines such as tumor necrosis factor- (TNF-), interleukin-1 (IL-1), IL-6 and interferon-gamma. It is currently in phase 2 trials for Myeloproliferative disorders, Polycythaemia vera and Phase III for Duchenne muscular dystrophy announced. In clinical trials of givinostat as a salvage therapy for advanced Hodgkin's lymphoma, the most common adverse reactions were fatigue, mild diarrhea or abdominal pain, moderate thrombocytopenia, and mild leukopenia.

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