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Restrict the search for
phenyl aminosalicylate
to a specific field?
Status:
Investigational
Source:
NCT01332266: Phase 1/Phase 2 Interventional Completed Platinum-Resistant Squamous Cell Carcinoma of the Head and Neck
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Golvatinib is a highly potent, small-molecule, ATP-competitive inhibitor of c-Met and multiple members of the Eph receptor family plus c-Kit and Ron. Eisai was developing an oral formulation of golvatinib, which acts as both a c-Met inhibitor and a vascular endothelial growth factor receptor 2 antagonist with potential antineoplastic activity. Golvatinib binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and VEGFR-2 are upregulated in a variety of various tumor cell types and play important roles in tumor cell growth, migration and angiogenesis. Clinical trials involving several forms of cancer are currently underway.
Status:
Investigational
Source:
NCT04103060: Phase 2 Interventional Completed Vitiligo
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Cerdulatinib is an oral, dual spleen tyrosine kinase (Syk) and janus kinase (JAK) inhibitor that uniquely inhibits two key cell signaling pathways that promote cancer cell growth in certain hematologic malignancies – the B-cell receptor pathway via Syk and key cytokine receptors via JAK Being developed to treat patients with hematologic cancers, specifically those who have relapsed or who have not responded to prior therapies. Cerdulatinib is in Phase 2 study evaluating the safety and efficacy of cerdulatinib in patients with relapsed/refractory B-cell malignancies who have failed multiple therapies.
Status:
Investigational
Source:
NCT01226277: Phase 1 Interventional Completed Solid Cancers
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
GDC-0917 (CUDC-427) is an orally available, monovalent mimetic of the second mitochondrial-derived activator of caspases (Smac/DIABLO) and inhibitor of IAPs (Inhibitor of Apoptosis Proteins) with potential antineoplastic activity. Smac mimetic GDC-0917 binds to the Smac binding groove on IAPs, including the direct caspase inhibitor X chromosome-linked IAP (XIAP) and the cellular IAPs 1 and 2. This inhibits the activities of these IAPs and promotes the induction of apoptosis through apoptotic signaling pathways. GDC-0917 demonstrated single-agent antitumor activity in mouse xenograft models bearing subcutaneous MDA-MB-231 tumors. In addition, CUDC-427 demonstrated additive activity in combination with chemotherapeutic agents and tumor necrosis factor apoptosis-inducing ligand (TRAIL) receptor targeting antibodies in xenograft tumor models. Preclinical safety and pharmacokinetic testing established an expected therapeutic range of doses as well as elucidated possible toxicities including inflammatory cytokine and chemokine proteins that could cause an inflammatory reaction, and reversible mild to moderate inflammation in the lungs and liver. GDC-0917 had been in phase I clinical trials by Genentech, Inc. for the treatment of Refractory Solid Tumors or Lymphoma. The principal toxicities related to CUDC-427 were mild to moderate in severity and included fatigue, nausea, vomiting, and rash.
Status:
Investigational
Source:
NCT00551811: Phase 1 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Elubrixin (SB-656933) is a CXCR2 antagonist that demonstrates dose-dependent effects on neutrophil activation and recruitment. In preclinical studies, the compound was shown to inhibit CXCL1-induced CD11b up-regulation on PMNs in an in vitro whole blood assay and to be active in in vivo rodent inhalation challenge models of airway inflammation that used endotoxin and ozone to induce airway neutrophilia. Elubrixin was being developed by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease, cystic fibrosis and ulcerative colitis. Elubrixin was withdrawn from the Phase II trial due to the lack of efficacy.
Status:
Investigational
Source:
NCT01154101: Phase 2 Interventional Completed Psoriasis
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
SRT2104, also known as GSK2245840, is a novel, first in class, highly selective small molecule activator of the NAD + dependent deacetylase SIRT1. SIRT1 has been suggested as putative therapeutic target in multiple age-related diseases including type 2 diabetes and dyslipidemias. SRT2104 in the phase II of clinical trial to treat type 2 diabetes mellitus and psoriasis also in the phase I for its use in case of colitis. Also was reported, that we report that SRT2104, penetrated the blood-brain barrier, attenuated brain atrophy, improved motor function, and extended survival in a mouse model of Huntington's disease.
Status:
Investigational
Source:
NCT02072863: Phase 1/Phase 2 Interventional Completed Multiple Myeloma
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Oprozomib (PR-047) is an orally bioavailable derivative of carfilzomib, with similar biological activity, i.e. inhibition of the chymotrypsin-like activity of the proteasome. It inhibits the activity of the proteasome, thereby blocking the targeted proteolysis normally performed by the proteasome; this may result in an accumulation of unwanted or misfolded proteins. Disruption of various cell signaling pathways may follow, eventually leading to the induction of apoptosis and inhibition of tumor growth. Oprozomib (PR-047) is being investigated for the treatment of hematologic malignancies, specifically, multiple myeloma, with Phase I/II trial ongoing.
Status:
Investigational
Source:
NCT02942771: Phase 1 Interventional Completed Healthy Adult Volunteers
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
TT-301 is a small molecule compound that has demonstrated efficacy in preclinical models of rheumatoid arthritis, intracerebral haemorrhage and traumatic brain injury. In preclinical studies, TT-301 has been shown to act by inhibiting the overproduction of inflammatory cytokines, such as interleukin-1 (IL-1Beta), tumour necrosis factor-alpha (TNF-Alpha), a key disease process associated with many inflammatory and degenerative diseases. TT-301 was designed to cross the blood-brain-barrier and has the flexibility to be administered by injection or orally. In preclinical studies to date, TT-301 has shown a favorable safety profile and a significant therapeutic benefit in animal models of disease. TT-301 has been used in trials studying the treatment of traumatic brain injury.
Status:
Investigational
Source:
NCT00417261: Phase 1 Interventional Completed Healthy
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02540876: Phase 1 Interventional Completed Metastatic Malignant Neoplasm
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Ilorasertib (previously known as ABT-348), an orally bioavailable ATP-competitive inhibitor of Aurora kinases (A, B and C), as well as the VEGF and PDGF families of receptor tyrosine kinases, was developed by AbbVie as an antineoplastic agent. It is known that Aurora kinases A, B, and C play essential roles in mitotic checkpoint control and are overexpressed by a wide variety of tumor cell types. Both VEGFRs and PDGFRs may be upregulated in various tumor cell types. Ilorasertib alone or in combination with azacitidine demonstrated activity in preclinical models in various hematological malignancies, indicating that pan-Aurora kinase and multiple kinase inhibition may have preferential antileukemic activity. Ilorasertib participated in phase I clinical for patients with advanced hematologic malignancies. The result has shown that the drug could be further studied in acute myelogenous leukemia. Ilorasertib is also going to be studied in phase II clinical trials to learn if this drug can help to control CDKN2A-deficient cancer in patients with advanced cancers.
Status:
Investigational
Source:
NCT01474941: Phase 1 Interventional Completed Healthy
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
PF-04620110 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that inhibits triacylglycerol synthesis in cells and in rodents. PF-04620110 inhibits DGAT-1 with an IC50 of 19 nM and shows high selectivity versus a broad panel of off-target pharmacologic end points. In vivo DGAT-1 inhibition has been demonstrated through reduction of plasma triglyceride levels in rodents at doses of ≥0.1 mg/kg following a lipid challenge. On the basis of this pharmacologic and pharmacokinetic profile, PF-04620110 has been advanced to human clinical studies. PF-4620110 had been in phase I clinical trials by Pfizer for the treatment of type 2 diabetes. But this research was discontinued in 2011.
![Structure of 1-[(2-Bromo-6-quinoxalinyl)methyl]-4-[4-(1-methylethyl)phenyl]-6-(2-propyn-1-yloxy)-2(1H)-quinazolinone](/img/3e2b89e2-59b0-48cd-bff1-b243d68cbc3a.svg?size=200&context=yfygkytiiu)
