crenigacestat

NOTCH1 inhibitor

Also Known As:

4,4,4-Trifluoro-N-((2S)-1-(((7S)-5-(2-hydroxyethyl)-6-oxo-6,7-dihydro-5H-pyrido(3,2-a)(3)benzazepin-7-yl)amino)-1-oxo-2-propanyl)butanamide; Butanamide, N-((1S)-2-(((7S)-6,7-dihydro-5-(2-hydroxyethyl)-6-oxo-5H-pyrido(3,2-a)(3)benzazepin-7-yl)amino)-1-methyl-2-oxoethyl)-4,4,4-trifluoro-; LY3039478

Networked: 24 relevant articles (2 outcomes, 13 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Benzazepines: 5
      - crenigacestat: 24

Experts

1.	Benhadji, Karim A: 5 articles (01/2021 - 11/2018)
2.	Massard, Christophe: 5 articles (01/2021 - 11/2018)
3.	Yuen, Eunice: 5 articles (01/2021 - 11/2018)
4.	Giannelli, Gianluigi: 3 articles (04/2022 - 01/2020)
5.	Mancarella, Serena: 3 articles (04/2022 - 01/2020)
6.	Serino, Grazia: 3 articles (04/2022 - 01/2020)
7.	Benhadji, K A: 3 articles (12/2020 - 01/2018)
8.	Armentano, Raffaele: 2 articles (04/2022 - 02/2022)
9.	Dituri, Francesco: 2 articles (04/2022 - 01/2020)
10.	Calvisi, Diego F: 2 articles (02/2022 - 01/2020)

Related Diseases

1.	Neoplasms (Cancer) 01/01/2017 - "Data from a phase I study indicate that LY3039478 is modestly effective against a range of advanced or metastatic cancers. " 10/01/2022 - "In the present study, a transcriptomic analysis approach, validated by Western blotting and qRT-PCR on iCCA tumor masses treated with Crenigacestat, was used to study the molecular pathways responsive to drug treatment. " 01/01/2018 - "In this first-in-human study, we report the safety, pharmacokinetic (PK) profile, pharmacodynamic effects, and antitumor activity of LY3039478 in patients with advanced or metastatic cancer. " 01/01/2018 - "First-in-human study of LY3039478, an oral Notch signaling inhibitor in advanced or metastatic cancer." 10/01/2022 - "Therefore, although these data need further investigation, our observations confirm that Crenigacestat selectively targets NOTCH1 and that the desmoplastic response in iCCA likely plays a key role in both drug effectiveness and tumor progression."
2.	Multiple Myeloma 01/01/2023 - "All-trans retinoic acid works synergistically with the γ-secretase inhibitor crenigacestat to augment BCMA on multiple myeloma and the efficacy of BCMA-CAR T cells." 07/01/2023 - "We aimed to evaluate the safety and identify the recommended phase 2 dose of BCMA CAR T cells in combination with crenigacestat (LY3039478) for individuals with relapsed or refractory multiple myeloma. "
3.	Disease Progression 01/01/2021 - "Methods The study consisted of 2 dose levels of crenigacestat (25 mg and 50 mg), administered orally 3 times per week (TIW) over a 28-day cycle until disease progression, development of unacceptable toxicity, or any other discontinuation criteria were met. " 01/01/2020 - "The ACC expansion cohort received the RP2D regimen of 50 mg crenigacestat thrice per week in a 28-day cycle until disease progression or other discontinuation criteria were met. " 11/01/2018 - "Eligible patients received LY3039478 50mg/75 mg three times per week, for 28-day cycle until disease progression. "
4.	Sarcoma (Soft Tissue Sarcoma) 11/01/2018 - "This phase 1a/b trial evaluated the safety, pharmacokinetics and antitumour activity of LY3039478 in patients with soft tissue sarcoma (STS) and gastrointestinal stromal tumour (GIST). " 11/01/2018 - "Notch pathway inhibition with LY3039478 in soft tissue sarcoma and gastrointestinal stromal tumours." 12/01/2020 - "Sequential treatment with NOTCH inhibitor crenigacestat followed by pazopanib in soft tissue sarcoma patients."
5.	Precursor Cell Lymphoblastic Leukemia-Lymphoma (Acute Lymphoblastic Leukemia) 01/01/2021 - "Phase 1 study to evaluate Crenigacestat (LY3039478) in combination with dexamethasone in patients with T-cell acute lymphoblastic leukemia and lymphoma."

Related Drugs and Biologics

1.	Amyloid Precursor Protein Secretases (beta-Secretase)
2.	bis(3- bis(4- chlorophenyl)methyl- 4- dimethylaminophenyl)amine
3.	Tretinoin (Retinoic Acid)
4.	crenigacestat
5.	Antineoplastic Agents (Antineoplastics)
6.	Gemcitabine
7.	Carboplatin (JM8)
8.	Prednisone (Sone)
9.	Dexamethasone (Maxidex)
10.	Cisplatin (Platino)

Related Therapies and Procedures

1.	Therapeutics