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Restrict the search for
vitamin a palmitate
to a specific field?
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:
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:
NCT02607280: Phase 3 Interventional Completed Diabetic Peripheral Neuropathic Pain
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Mirogabalin, a selective alpha 2 delta ligand binds to the α2δ subunits of voltage-dependent calcium channels and thus blocks the channel. This drug was developed by Daiichi Sankyo and in January 2019 was approved in Japan for the treatment of neuropathic pain and for the postherpetic neuralgia.
Status:
Investigational
Source:
NCT02335814: Phase 1 Interventional Terminated Acute Myeloid Leukemia
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
AMG-925, a dual FLT3/CDK4 inhibitor, has been developed to overcome resistance to FLT3 inhibitors, which is a serious clinical issue in treating acute myelogenous leukemia (AML). AMG-925 inhibits FLT3, including many FLT3 mutants reported to date. AMG-925 inhibits the proliferation of a panel of human tumor cell lines including Colo205 (Rb(+)) and U937 (FLT3(WT)) and induced cell death in MOLM13 (FLT3(ITD)) and even in MOLM13 (FLT3(ITD, D835Y)), which exhibits resistance to a number of FLT3 inhibitors currently under clinical development. At well-tolerated doses, AMG-925 leads to significant growth inhibition of MOLM13 xenografts in nude mice, and the activity correlates with inhibition of STAT5 and Rb phosphorylation. AMG-925 is in Phase I clinical trials for the treatment of Acute myeloid leukaemia.
Status:
Investigational
Source:
NCT00297180: Phase 2 Interventional Completed Obesity
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sergliflozin, a novel oral selective low-affinity sodium glucose cotransporter (SGLT2) inhibitor, improves hyperglycemia by suppressing renal glucose reabsorption, in which SGLT2 participates as a dominant transporter. Its prodrug form, sergliflozin etabonate, is orally available and is converted to sergiflozin upon absorption. Development of sergliflozin has been discontinued in favor of remogliflozin.
Status:
Investigational
Source:
NCT02603445: Phase 1 Interventional Completed Follicular Lymphoma, Mantle Cell Lymphoma
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT04150042: Phase 1 Interventional Recruiting Pancreatic Adenocarcinoma Metastatic
(2021)
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
Status:
Investigational
Source:
NCT03559192: Phase 2 Interventional Completed Depressive Disorder, Major
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
LY-2456302 or CERC-501 (now JNJ-67953964) is a non-peptide, centrally-penetrant, potent, short-acting kappa opioid receptor (KOR)-selective antagonist with pharmacokinetic properties favorable for clinical development and activity in animal models predictive of efficacy in mood and addictive disorders. It is under development for depression and substance abuse disorders.
Status:
Investigational
Source:
NCT03620474: Phase 1/Phase 2 Interventional Completed Hepatitis C
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
