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Restrict the search for
tyrosine
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Status:
Investigational
Source:
NCT03725722: Phase 2 Interventional Completed Atopic Dermatitis
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT03230318: Phase 2 Interventional Completed Intrahepatic Cholangiocarcinoma
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Derazantinib (ARQ 087) is an investigational, oral, multi-kinase inhibitor designed to preferentially inhibit the FGFR family of kinases with demonstrated activity in FGFR2 genetic alterations, including fusions. In human cancers, FGFRs have been found to be dysregulated by multiple mechanisms, including aberrant expression, mutations, chromosomal rearrangements, and amplifications. FGFR dysregulation has been identified as a driver in a number of cancers, including iCCA, cholangiocarcinoma, bladder, endometrial, breast, gastric, lung and ovarian. Current scientific literature suggests FGFR alterations exist in anywhere from 5% to 40% of these cancers. Derazantinib is a potent FGFR inhibitor that shows strong anti-proliferative activity in cell lines harboring FGFR2 alterations. In clinical testing, the molecule has demonstrated activity in cancerous tumors harboring FGFR2 fusions in iCCA and bladder cancers.
Status:
Investigational
Source:
NCT03099148: Phase 1 Interventional Completed Healthy
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01297088: Phase 1 Interventional Completed Diagnostic Imaging
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
BAY-86-9596 (D-18F-FMT, or O-18F-fluoromethyl-D-tyrosine) was developed as an agent not only for tumor detection but also for monitoring early-phase response to radiation therapy by positron emission tomography (PET). This drug participated in clinical trials for patients with inflammation and solid tumors, but further information about trials is not available.
Status:
Investigational
Source:
NCT03906071: Phase 3 Interventional Active, not recruiting Metastatic Non-Squamous Non-Small Cell Lung Cancer
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Sitravatinib (MGCD516) is a receptor tyrosine kinases (RTK) inhibitor that blocks a wide array of RTKs known to be amplified/overexpressed in sarcomas, which are key regulators of signaling pathways that lead to cell growth, survival and tumor progression. It is involved in driving sarcoma cell growth with IC50 of 3980 nM and is superior to other multi-kinase inhibitors in inhibiting cell proliferation, RTK phosphorylation, and phosphorylation of downstream effectors. The efficacy of sitravatinib was tested using a wide panel of sarcoma cell lines, including malignant peripheral nerve sheath tumor (MPNST), Ewing sarcoma (A673), osteosarcoma (Saos2), and liposarcoma (DDLS, LS141). Both in vitro and in vivo efficacy sitravatinib was significantly better that the other two multi-kinase inhibitors, imatinib and crizotinib. Sitravatinib treatment not only inhibits tumor cell proliferation at low nanomolar concentrations in vitro but also results significant tumor growth suppression in vivo in mouse xenograft models. Sitravatinib is being evaluated in a Phase 1b dose expansion cohort in selected patients with specific genetic alterations that are drivers of tumor growth, with an initial focus on Non-Small-Cell Lung carcinoma (NSCLC) and in other solid tumors where sitravatinib may confer a benefit. Its efficacy and safety is also being tested in Phase II clinical trials in patients with advanced liposarcoma as a monotherapy and NSCLC in combination with nivolumab.
Status:
Investigational
Source:
NCT02228811: Phase 1 Interventional Terminated Locally Advanced Tumors
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Altiratinib, a novel c-MET/TIE-2/VEGFR inhibitor, was able to effectively reduce tumor burden in vivo and block c-MET signaling, cell growth and migration. Altiratinib inhibits not only mechanisms of tumor initiation and progression, but also drug resistance mechanisms in the tumor and microenvironment. Altiratinib durably inhibits MET, both wild-type and mutated forms, in vitro and in vivo. Altiratinib exhibits properties amenable to oral administration and exhibits substantial blood-brain barrier penetration, an attribute of significance for eventual treatment of brain cancers and brain metastases. It is currently in Phase 1 clinical development for the treatment of solid tumors.
Status:
Investigational
Source:
NCT01496495: Phase 1 Interventional Completed Myelodysplastic Syndromes
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with potential antineoplastic, anti-inflammatory and antiangiogenic activities. Pexmetinib inhibited leukemic proliferation, prevented activation of downstream effector kinases and abrogated the effects of TNF-alpha on healthy hematopoietic stem cells. In ex vivo stimulated human whole blood, LPS-induced cytokines was inhibited by Pexmetinib with an IC50 value ranging from 50-120 nM. ARRY-614 inhibited the release of IL-6 from SEA- or LPS-challenged mice with an ED50 value less than 10 mg/kg. Combining Pexmetinib with lenalidomide inhibited both pro-inflammatory cytokines and tumor growth in vivo with higher potency, compared with either agent alone. In dose escalation or expansion cohorts, treatment with Pexmetinib either once daily or twice daily was applied to forty-five patients. Pexmetinib reduced the levels of circulating biomarkers and the p38 MAPK activation of bone marrow.
Status:
Investigational
Source:
NCT03100942: Phase 2 Interventional Completed Sjogren's Syndrome
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Tirabrutinib (also known as ONO-4059 or GS-4059), a second-generation, enhanced-selectivity Bruton's tyrosine kinase inhibitor that demonstrated antitumor activity in preclinical models. Tirabrutinib participated in phase I clinical trial in patients with relapsed or refractory B-cell malignancies, where it was well tolerated and showed promising efficacy. In addition, tirabrutinib is involved in phase II clinical trials to study safety and efficacy in adults with Active Sjogren's syndrome and in adults with chronic lymphocytic leukemia. Besides the drug was studied for the treatment of Waldenstrom's macroglobulinemia and patients with refractory pemphigus.
Status:
Investigational
Source:
NCT04092452: Phase 2 Interventional Completed Acne Inversa
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
PF-06700841 is an inhibitor of JAK1 and TYK2 kinases. PF-06700841 tosylate salt is potentially a treatment of systemic lupus erythematosus and plaque psoriasis.
Status:
Investigational
Source:
NCT03824080: Phase 2 Interventional Completed Acute Myeloid Leukemia
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM. R428 was originated in Rigel Pharmaceuticals and was licensed to BerGenBio, which initiated clinical trials for the treatment of non-small cell lung cancer, metastatic melanoma and acute myeloid leukaemia.
