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Restrict the search for
methyl salicylate
to a specific field?
Status:
Investigational
Source:
NCT02445976: Phase 2 Interventional Completed Prostate Cancer
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Seviteronel (VT-464) is a 17,20-lyase selective inhibitor of CYP17A1, which plays key roles in adrenal and intratumoral de novo biosynthesis of androgens. The inhibition of 17,20-lyase activity by seviteronel (VT-464) is enough to reduce androgen levels, and its preserving of 17alpha-hydroxylase activity largely avoids interference with the production of other steroidal hormones. Seviteronel (VT-464) also has shown AR-antagonist activity independent of CYP17 enzyme inhibition. It is currently in phase 2 clinical trials as a therapeutic for castration-resistant prostate cancer patients.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT03997838: Phase 3 Interventional Completed Pain, Postoperative
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
INN:lerimazoline [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Lerimazoline is a sympathomimetic drug that belongs to the imidazoline class of compounds, and is used as a nasal decongestant. Lerimazoline displayed high affinity for the 5-HT1A receptor and for the 5-HT1D receptor. Binding affinity estimates for α1-adrenoceptor, 5-HT2A, and D2 receptors were more than ten times lower. The mechanism of vasoconstrictor action of lerimazoline encompasses both, the activation of 5-HT2A, and to a lesser degree α1 -adrenergic receptors. These results also suggest that lerimazoline is an “atypical” decongestant. It inhibits secretion of nasal mucus. Lerimazoline causes hypertension.
Status:
Investigational
Source:
NCT02518113: Phase 1/Phase 2 Interventional Completed T-cell Acute Lymphoblastic Leukemia
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
LY-3039478 is an orally bioavailable, novel small molecule inhibitor of Notch signaling pathway, developed Eli Lilly and Company for cancer treatment. The Notch receptor, on the surfaces of progenitor cells and cancer cells, binds neighboring cell-surface ligands DLL or JAGGED. On ligand binding, the intramembrane protease γ-secretase cleaves the Notch intracellular domain (NICD). LY-3039478 is an exquisitely potent inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with an IC50 of ∼1nM in most of the tumor cell lines tested. LY3039478 also potently inhibits mutant Notch receptor activity. Treatment with a gamma-secretase inhibitor, LY3039478, significantly inhibited the growth of 2 CCRCC(Clear cell renal cell carcinoma) cell lines in a concentration-dependent manner. LY3039478 treatment also led to decreased expression of Myc and Cyclin A1, two genes that were part of the NOTCH driven proliferative signature in murine and human model systems. LY3039478 treatment also led to G0/G1 cell cycle arrest in CCRCC cells. In a xenograft tumor model, LY3039478 inhibited N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment. The inhibition of Notch cleavage also resulted in the induction of apoptosis in a Notch-dependent xenograft model. In immunodeficient NSG mice xenografted with 769-P CCRCC cells, LY3039478 treatment resulted in significantly increased survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC. LY3039478 is being investigated in a clinical trial in patients with T-cell acute lymphoblastic leukemia or T-cell lymphoblastic lymphoma in combination with Dexamethasone.
Status:
Investigational
Source:
NCT01673737: Phase 1 Interventional Completed Neoplasm Malignant
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Sanofi has developed SAR260301 as a selective inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) beta isoform with potential antineoplastic activity. It is known that the dysregulation of the PI3K/Akt/mTOR pathway is frequently found in solid tumors and contributes to increased tumor cell growth, tumor cell survival. SAR260301 participated in phase I clinical trials in patients with advanced solid tumors. It was found that the drug had an acceptable safety profile, but exposure sufficient to inhibit the PI3K pathway was unachievable because of rapid clearance, and clinical development was terminated.
Status:
Investigational
Source:
INN:aramisulpride [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT03731026: Phase 3 Interventional Unknown status Breast Cancer
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT02722018: Phase 1 Interventional Completed Healthy Volunteer
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
ARN-810 (GDC-0810) is a novel, orally bioavailable, estrogen receptor antagonist that induces proteasomal estrogen receptor degradation in breast cancer cell lines at picomolar concentrations and tumor regression in tamoxifen-sensitive and resistant BC xenograft models. Results from a first-in-human phase I/IIa study of ARN-810 indicate that it is tolerable and may benefit some postmenopausal women with advanced estrogen receptor-positive breast cancer. Development of ARN-810 was discontinued.
Status:
Investigational
Source:
INN:lexanopadol [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Lexanopadol is a potent ORL-1 agonist (opioid receptor like -1), nociceptin receptor agonists and opioid mu receptor agonists. Preliminary evidence suggests that targeting ORL-1 receptors may have synergistic effects with mu receptors hence enhancing the therapeutic profile of Lexanopadol in the treatment of pain. Lexanopadol is particularly suited for the management of moderate to severe chronic pain, including neuropathic pain. Lexanopadol hemicitrate is in phase II clinical trials for the treatment of pain. However there is no recent development reported.
