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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Source:
INN:bamirastine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Bamirastine (previously known as TAK 427), an antiallergic compound that inhibits ligand binding to recombinant human histamine H1 receptor. The drug was involved in phase II clinical trials for the treatment of allergic rhinitis and for patients with atopic dermatitis. However, these studies were discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Exisulind (tentative trade name Aptosyn) is an antineoplastic agent, which was originally developed by Cell Pathways. This drug is an inhibitor of phosphodiesterase (PDE) isozymes: PDE5 and PDE4. Inhibition of PDE5 appears to be pharmacologically relevant, which leads to increase cGMP and activate protein kinase G at doses that induce apoptosis, whereas cyclic AMP levels were not changed. Exisulind has been in phase III clinical trials for the treatment of Non-Small Cell Lung Cancer and for the treatment of polyps in patients who have familial adenomatous polyposis (Colorectal Cancer and Small Intestine Cancer). In addition, this drug was in phase II/III for the treatment of Prostate Cancer, however, there studies have been discontinued.
Status:
Investigational
Source:
INN:morphine glucuronide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Morphine-6-glucuronide is a pharmacologically active metabolite of morphine that is being developed by CeNeS Pharmaceuticals as an alternative to morphine for the management of postoperative pain. Compared to morphine, Morphine-6-glucuronide has been reported to have6 and 86 times lower affinity for the human mu and kappa opioid receptors, respectively, and similar affinity for the delta opioid receptor. Morphine-6-glucuronide is was studied in phase III clinical trials for postoperative pain management. Unfortunately, Morphine-6-glucuronide failed to demonstrate superior safety compared to Morphine and further development was discontinued. Morphine-6-glucuronide accumulates after administration of morphine to patients with renal insufficiency, and analgesia can be obtained with lower doses of morphine compared to patients with normal renal function. More importantly, the dose should be reduced to avoid serious side-effects, although the simulations in this review did not account for side-effects.
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Darglitazone is a member of the thiazolidinedione class of drugs and an agonist of peroxisome proliferator-activated receptor-γ (PPAR-γ), an orphan member of the nuclear receptor superfamily of transcription factors. It has a variety of insulin-sensitizing effects, such as improving glycemic and lipidemic control, and is used in the treatment of metabolic disorders such as type II diabetes. Darglitazone sodium had been in phase I clinical trials by Pfizer for the treatment of type 2 diabetes. However, this study has been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Otenabant (CP-945,598) is Pfizer developed as a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, which exhibits 10,000-fold greater selectivity against human CB2 receptor, for treatment of obesity. In clinical trial III Pfizer decided to discontinue the development program based on changing regulatory perspectives on the risk/benefit profile of the CB1 class and likely new regulatory requirements for approval.
Status:
Investigational
Source:
INN:iometopane (¹²³I) [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Iometopane I-123 is a tropane derivative labeled with iodine-123 that was being developed by MGI GP (MGI Pharma) as an injectable Single-photon emission computed tomography (SPECT) imaging agent. The ability of iometopane to bind to the dopamine transporter on presynaptic dopaminergic nerve terminal in the striatum has been used to differentiate the uptake of the agent by the neurons in the striatum in patients with a Parkinsonian disorder from patients without a Parkinsonian disorder with high sensitivity and specificity. The diminished uptake of iometopane in the striatum on the SPECT images of patients with a Parkinsonian disorder can be applied to assess both disease trait and disease state (severity) reflected by the severity of the brain dopamine neuron loss. Unfortunately Phase III clinical trials and further development of iometopane was discontinued due to the inability to contract a suitable manufacturer for the clinical and commercial supply of iometopane on acceptable conditions in the US. Currently, Iometopane is mainly used in scientific research into the dopamine reuptake transporter.
Status:
Investigational
Source:
INN:zosurabalpin [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Class (Stereo):
CHEMICAL (ACHIRAL)
Pheneridine is a synthetic opioid. It was developed as a narcotic agent.
Class (Stereo):
CHEMICAL (RACEMIC)
Talmetacin is a cyclo-oxygenase inhibitor that was studied as an analgesic and antipyretic agent. This drug was studied in Argentina in patients with rheumatic disorders. However, further development of talmetacin is not available.
Status:
Investigational
Source:
NCT03756103: Phase 2 Interventional Completed Hypertension,Essential
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
