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Showing 1531 - 1540 of 24164 results

Status:
Investigational
Source:
NCT01530529: Phase 1 Interventional Completed Healthy
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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:
INN:fosgonimeton [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03838185: Phase 1 Interventional Completed Alzheimer's Disease
(2019)
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.
PF-05089771 is an oral administrated Nav1.7 channel inhibitor. PF-05089771 provided the best opportunity to explore Nav1.7 blockade for the treatment of acute or chronic pain conditions. PF-05089771 has completed Phase II clinical trials of third molar extraction and primary inherited erythromelalgia. The magnitude of efficacy of PF-05089771 in the randomized, placebo-controlled, double-blind clinical study in subjects with painful diabetic peripheral neuropathy was disappointing. Although there was a trend towards a reduction in pain and improvement in sleep rating in patients with painful DPN when compared to placebo treatment, this was not statistically significant.
Status:
Investigational
Source:
NCT03660059: Phase 3 Interventional Completed Rheumatoid Arthritis (RA)
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Peficitinib (formerly known as ASP015K) is a pyrrolo[2,3-b]pyridine derivative orally administered once-daily JAK inhibitor in development for the treatment of Rheumatoid Arthritis. In preclinical studied Peficitinib inhibited JAK1 and JAK3 with IC50 of 3.9 and 0.7 nM, respectively. Peficitinib also inhibited IL-2-dependent T cell proliferation in vitro and STAT5 phosphorylation in vitro and ex vivo. Furthermore, Peficitinib dose-dependently suppressed bone destruction and paw swelling in an adjuvant-induced arthritis model in rats via prophylactic or therapeutic oral dosing regimens.In clinical trials, Peficitinib treatment prescribed at 50, 100 and 150 mg amounts each showed statistically significantly higher ACR20 response rates compared to the placebo and response rates increased up to the 150 mg dosage. Adverse events included neutropenia, headache, and abdominal pain. The treatment-emergent adverse events occurring more frequently in the Peficitinib group compared with the placebo group included diarrhea, nasopharyngitis, and increased serum creatine phosphokinase activity. No cases of serious infections were reported. Herpes zoster occurred in four patients (two each in the peficitinib 25 and 100 mg cohorts). The authors concluded that treatment with peficitinib as monotherapy for 12 weeks in Japanese patients with moderate to severe RA is efficacious and showed an acceptable safety profile.
I-BET-762 (GSK 525762) is a small molecule benzodiazepine, by 'mimicking' acetylated histones interferes with the recognition of acetylated histones by BET family of bromodomains (BRD2, BRD3, and BRD4), which disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumour cell growth. GlaxoSmithKline is developing GSK 525762 for the oral treatment of solid tumours and haematological malignancies.
Status:
Investigational
Source:
NCT00752830: Phase 1 Interventional Completed Healthy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

AZD0328, a spirofuropyridine, is a selective alpha7 nicotinic receptor agonist. This drug participated in clinical trials phase II in patients with schizophrenia. However, studies were terminated because the drug didn’t meet the current target product profile. Besides AZD0328 has been studied in phase I for the treatment of Alzheimer's disease.
Status:
Investigational
Source:
NCT01260480: Phase 2 Interventional Unknown status Carcinoma, Non-Small-Cell Lung
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Showing 1531 - 1540 of 24164 results