H3B-8800

an orally available small-molecule splicing modulator

Also Known As:

(2S,3S,4E,6S,7R,10R)-7,10-dihydroxy-3,7-dimethyl-12-oxo-2-((2E,4E,6R)-6-(2-pyridinyl)-2,4-heptadien-2-yl)oxacyclododec-4-en-6-yl 4-methyl-1-piperazinecarboxylate; 1-piperazinecarboxylic acid, 4-methyl-, (2S,3S,4E,6S,7R,10R)-7,10-dihydroxy-3,7-dimethyl-2-((1E,3E,5R)-1-methyl-5-(2-pyridinyl)-1,3-hexadien-1-yl)-12-oxooxacyclododec-4-en-6-yl ester

Networked: 10 relevant articles (0 outcomes, 3 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyridines: 88
    - H3B-8800: 10
  - Piperazines: 26
    - H3B-8800: 10

Experts

1.	Taylor, Justin: 2 articles (12/2021 - 01/2018)
2.	Yao, Huilan: 2 articles (12/2021 - 01/2018)
3.	Smith, Peter G: 2 articles (09/2020 - 01/2018)
4.	Zhu, Ping: 2 articles (01/2020 - 01/2018)
5.	Ades, Lionel: 1 article (12/2021)
6.	Al-Kali, Aref: 1 article (12/2021)
7.	Alfonso-Piérola, Ana: 1 article (12/2021)
8.	Alonso-Dominguez, Juan M: 1 article (12/2021)
9.	Brunner, Andrew M: 1 article (12/2021)
10.	Carraway, Hetty E: 1 article (12/2021)

Related Diseases

1.	Neoplasms (Cancer) 12/01/2021 - "Phase I First-in-Human Dose Escalation Study of the oral SF3B1 modulator H3B-8800 in myeloid neoplasms." 11/18/2020 - "H3B-8800 had unique pharmacological activity and exhibited favorable data in phase I clinical trials to treat patients with advanced myeloid malignancies, indicating that further clinical trials are promising. " 10/18/2021 - "This supports the hypothesis that the selectivity of H3B-8800 towards mutant cancer cells is unrelated to its preferential targeting of K700ESB3b. " 10/18/2021 - "Among these, H3B-8800 is of particular interest, as it induces preferential lethality in cancer cells bearing the frequent and highly pathogenic K700E SF3B1 mutation. " 09/30/2021 - "The potential of pladienolides as anti-cancer agents is confirmed by H3B-8800, a synthetic analog of this natural product class, which is currently under Phase I clinical trials. "
2.	Hematologic Neoplasms (Hematological Malignancy) 01/01/2021 - "Its utility is further demonstrated by the enantioselective total synthesis of H3B-8800, a hitherto semisynthetic pladienolide-derived spliceosome modulator undergoing clinical trials for hematological malignancies."
3.	Precursor T-Cell Lymphoblastic Leukemia-Lymphoma (T-ALL) 01/01/2020 - "The splicing inhibitor H3B-8800 affects splicing of proteasomal transcripts and proteasome activity and acts synergistically with proteasome inhibitors in inhibiting T-ALL growth. "
4.	Leukemic Infiltration 11/01/2023 - "Using the H3B-8800 splicing modulator, we show, for the first time in CLL, cytotoxic effects in vitro in primary CLL samples and in SF3B1-mutated isogenic CLL cell lines, accompanied by major splicing changes and delayed leukemic infiltration in a CLL xenotransplant mouse model. "
5.	B-Cell Chronic Lymphocytic Leukemia (Chronic Lymphocytic Leukemia) 11/01/2023 - "SF3B1 mutation-mediated sensitization to H3B-8800 splicing inhibitor in chronic lymphocytic leukemia."

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