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Status:
Investigational
Source:
Eur J Cancer Clin Oncol. May 1986;22(5):601-5.: Phase 2 Human clinical trial Completed Breast Neoplasms
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Carubicin (also known as Carminomycin) is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. The drug is active against a variety of experimental tumors. Pharmacology studies in animals revealed that the drug bound largely to serum proteins and that it was widely distributed. In clinical trials The main toxic effect was myelosuppression but gastrointestinal intolerance and alopecia were also reported. Objective partial responses were seen in two of seven previously untreated patients with non-small cell lung cancer and one of three patients with squamous cell carcinoma of the head and neck previously untreated with chemotherapy.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Algestone is a progesterone like female hormone. Algestone is a C21-steroid that is pregn-4-ene substituted by oxo groups at position 3 and 20 and hydroxy groups at positions 16 and 17. It has a role as a progestin. It is a 20-oxo steroid, a 16alpha-hydroxy steroid, a 17-hydroxy steroid, a C21-steroid, a 3-oxo-Delta(4) steroid and a tertiary alpha-hydroxy ketone. It derives from a hydride of a pregnane. Algestone is used as anti-inflammatory drug (topical) and combination with enanthate as injectable contraceptive.
Status:
Investigational
Source:
NCT02253342: Phase 1 Interventional Completed Intrapulmonary Pharmacokinetics of WCK 2349
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Levonadifloxacin is the S-(-) isomer of the benzoquinolizine fluoroquinolone nadifloxacin and is two- to four-fold more active than the racemic mixture. Levonadifloxacin is a potent antibacterial agent against Gram-positive bacteria especially against methicillin resistance Staphylococcus aureus. It also possesses potent bactericidal activity against other resistant variants like quinolone-resistant Staphylococcus aureus, vancomycin and glycopeptide intermediate Staphylococcus aureus and vancomycin resistant Staphylococcus aureus. Intravenous dosage form developed to treat complicated skin and skin structure infections and has recently completed Phase III studies in India and Phase I studies in USA.
Status:
Investigational
Source:
JAN:ROTRAXATE HYDROCHLORIDE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Rotraxate (also known as TEI 5103 or TG 51) is an anti-ulcerative agent. Experiments on rodents have shown that only the oral and gastric route of administration lead to the anti-ulcer effect. This drug increased gastric mucosal blood flow and possibly promoted the healing process of peptic ulcers. However, the further development of this drug was discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Clinafloxacin is a broad-spectrum fluoroquinolone antibiotic that was originally developed and subsequently abandoned in the late 1990s as a human health antibiotic for respiratory diseases. Clinafloxacin displays broad-spectrum antibacterial activity against Gram-positive, Gram-negative, and anaerobic pathogens by inhibiting the bacterial regulatory enzyme DNA gyrase (IC50 = 0.92 ug/ml) as well as topoisomerase IV (IC50 = 1.62 ug/ml).
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Salacetamide is a derivative of salicylic acid. It is analgesic, anti-inflammatory and antipyretic agent.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Desomorphine is the common name for 4,5--epoxy-17- methylmorphinan-3-ol or dihydrodesoxymorphine-D. It is an opioid analogue and morphine derivative in which the 6-hydroxyl group and the double bond at carbons 7 and 8 of morphine are reduced. Desomorphine can cross the blood–brain barrier, binding to opioid receptors, similar to the pharmacokinetic distribution of all phenanthrene-structured alkaloids. Taking Desomorphine causes euphoria as well as sedative and analgesic relief. In addition to its faster onset than other powerful painkillers drugs such as morphine, desomorphine also initiates less sedative effects and seems to have favorable postoperative results, such as reduced need for catheterization, less dizziness, and decreased vomiting incidence. In comparison with Morphine, Desomorphine is faster reduced. It follows that it has to be taken it more frequently to get the same effects. Furthermore, it causes side effects such as respiratory and gastrointestinal problems and increased blood pressure. In addition, Desomorphine’s withdrawal symptoms are up to three times longer than Morphine’s. This leads to the conclusion that Desomorphine is more addictive. At present, desomorphine is classified as a narcotic drug (DEA code number 9055) in Schedule I of the U.S. Controlled Substances Act and is listed as a controlled substance under the international Single Convention on Narcotic Drugs of 1961.
Class (Stereo):
CHEMICAL (ACHIRAL)
The nitrofuran derivative, nifurprazine, is a topical antibacterial agent used mainly for the treatment of animal diseases. It is a trypanocidal drug. Nifurprazine proved to be the most promising derivative since it was redox-cycled by both T. cruzi LipDH and TR and had pronounced antiparasitic effects in cultures of T. cruzi and Trypanosoma brucei.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Droloxifene, a derivative of the triphenylethylene drug tamoxifen, is a novel selective estrogen receptor modulator (SERM). Droloxifene also exhibits more rapid pharmacokinetics, reaching peak concentrations and being eliminated much more rapidly than tamoxifen. Its higher affinity to the estrogen receptor, higher anti-estrogenic to estrogenic ratio, more effective inhibition of cell growth and division in estrogen receptor-positive cell lines, and lower toxicity give it theoretical advantages over tamoxifen in the treatment of human breast cancer. Short-term toxicity was generally mild, and similar to that seen with other antiestrogens. Droloxifene appears active and tolerable. It may have a particular role in situations in which rapid pharmacokinetics, or an increased antiestrogenic to estrogenic ratio, are required. Droloxifene may also be a potentially useful agent for the treatment of postmenopausal osteoporosis because it can prevent estrogen deficiency-induced bone loss without causing uterine hypertrophy. Droloxifene may have an effect on bone and breast tissue because it induces apoptosis. Droloxifene has an anti-implantation effect in rats, and the effect appears to be not completely due to its anti-estrogenic activity.
Status:
Investigational
Source:
INN:tomoxiprole [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tomoxiprole belongs to the class of 3-alkyl-2-aryl-3H-naphth (1,2-d)imidazoles. It is a nonsteroidal anti-inflammatory compound that was reported to have low ulcerogenic potential. Tomoxiprole inhibition of cyclooxygenase-2 but not cyclooxygenase-1 is time-dependent. It has anti-inflammatory activity in various anti-inflammatory models such as carrageenin and nystatin oedemas, cotton pellet granuloma and adjuvant arthritis. The anti-inflammatory potency of tomoxiprole is greater than that of acetylsalicylic acid and phenylbutazone, but lower than that of indomethacin. Tomoxiprole reduced PGE2 and 6-keto-PGF1 alpha levels more effectively in inflamed tissue than in gastric mucosa when assayed in in vivo experiments, whereas indomethacin and other non-steroidal anti-inflammatory drugs are equally effective in both systems.