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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Source:
INN:florilglutamic acid (¹⁸F) [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
FLORILGLUTAMIC ACID F-18 is a radioactive L-glutamate derivative and a tumor-specific positron emission tomography (PET) tracer. Orphan designation (EU/3/16/1632) was granted by the European Commission to Piramal Imaging GmbH, Germany, for FLORILGLUTAMIC ACID F-18 for the diagnosis of hepatocellular carcinoma. Currently, it is in phase II trial as a PET tracer in early lung cancer in patients with lung nodules.
Status:
Investigational
Source:
INN:iofolastat (¹²³I) [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Iofolastat I-123 is a radiolabeled iodobenzylamine derivative developed by Molecular Insight Pharmaceuticals, Inc as molecular imaging pharmaceuticals for prostate cancer. Iofolastat I123 selectively binds prostate-specific membrane antigen (PSMA), which allows imaging of PSMA-expressing prostate cancer cells. In Phase I clinical trial Iofolastat I-123 localized to lesions in bone and soft tissue that correlated with radiologic evidence of metastatic prostate cancer. Minimal uptake of one of Iofolastat I-123 as seen in the prostate gland of healthy volunteers, suggesting the possibility of visualizing disease in that organ.
Status:
Investigational
Source:
NCT02043899: Phase 1/Phase 2 Interventional Completed Metastatic Neuroblastoma
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ravidasvir (RDV, ASC16) is a second‐generation, pan‐genotypic non‐structural (NS) 5A inhibitor, which inhibits viral replication and assembly. Ravidasvir exhibits high antiviral potency with EC50 0.04–1.14 nM for HCV GT1–GT6. The pharmacokinetics results indicated that steady status achieved quickly after the first dose. Metabolism studies utilizing human clinical samples showed that Ravidasvir was very stable, with only modest (~2%) metabolite formation. Biliary excretion of Ravidasvir appears to be the primary route of elimination of the absorbed dose, while renal excretion of the intact drug appears to be negligible. In clinical trans twelve-week Ravidasvir and ritonavir-boosted Danoprevir in combination with ribavirinfor 12 weeks achieve the sustained virologic response rate of 100% in treatment-naïve non-cirrhotic Asian patients with HCV GT1 infection. Ravidasvir for treatment‐naïve, non‐cirrhotic HCV GT1 patients was safe and well tolerated. There was no death, treatment‐related serious adverse events, and discontinued cases due to adverse events.
Status:
Investigational
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:
NCT01445860: Phase 1 Interventional Completed Human Volunteers
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Pfizer was developing PF-3882845, an orally available nonsteroidal antagonist of the mineralocorticoid receptor, for the treatment of diabetic nephropathies. PF‐03882845 is a highly potent (IC50 = 6.3‐13.4 nM, 10% fetal bovine serum & IC50 = 0.504–1.11 nM, absence of serum) selective orally bioavailable mineralocorticoid receptor antagonist. It is a non‐steroidal pyrazoline, unlike steroidal compounds eplerenone and spironolactone. It does not significantly activate or inhibit human androgen receptor, estrogen receptor alpha, and glucocorticoid receptor. PF‐03882845 has been shown to modestly inhibit the progesterone receptor (PR) yielding a 45‐fold selectivity over PR in a cell‐based functional assay. PF‐03882845 was previously in development for the treatment of diabetic nephropathy — development for this indication was terminated for strategic reasons. An alternative indication of hypertension also was not pursued for strategic reasons.
Class (Stereo):
CHEMICAL (ACHIRAL)
Benfosformin (also known as JAV 852), a phosphorylated biguanide that was studied as a hypoglycemic and antidiabetic agent. However, the information about the studies of this compound now is not available.
Status:
Investigational
Source:
JAN:CARPIPRAMINE MALEATE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Viquidacin (also known as NXL-101), a quinoline antibacterial agent, was studied as a bacterial DNA gyrase and topoisomerase IV inhibitor. Viquidacin showed potent activity against gram-positive bacteria, including methicillin- and fluoroquinolone-resistant strains. The drug participated in phase I clinical trial. Viquidacin achieved homogeneous and potent bactericidal concentrations in human volunteer plasma. However, further, development was discontinued after QT interval prolongation, which was observed in a healthy volunteer.
Status:
Investigational
Source:
JAN:DELEOBUVIR SODIUM [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Deleobuvir is a drug for the treatment of Hepatitis C, developed by Boehringer Ingelheim. Deleobuvir is a non-nucleoside HCV NS5B polymerase inhibitor that reversibly and noncovalently binds to the thumb pocket 1. It has shown rapid and strong antiviral activity when administered in combination with peginterferon-a2a and ribavirin. In 2014 Boehringer Ingelheim decided to halt further development of deleobuvir because preliminary analysis of phase 3 clinical trials indicated a low efficacy of the drug.
