U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 141 - 150 of 282 results

Status:
Possibly Marketed Outside US
Source:
MIRIPLA by Dainippon Sumitomo Pharma
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Miriplatin is a novel lipophilic platinum complex that was developed to treat hepatocellular carcinoma (HCC). Miriplatin hydrate was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on Oct 16, 2009. It was developed and marketed as Miripla® by Dainippon Sumitomo Pharma on Jan 20, 2010 in Japan. Miriplatin hydrate is a lipophilic platinum complex that has high affinity to lipiodol. It is indicated for the treatment of transcatheter arterial chemoembolization of hepatocellular carcinoma. Miripla® is available as lyophilized powder for arterial injection, containing 70 mg of free Miriplatin. The recommended dose is 70 mg once daily.
Status:
Possibly Marketed Outside US
Source:
Mustargen by Gilman, A.|Goodman, L.S.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Mechlorethamine Oxide was approved by the FDA in 1949 for the treatment of hematologic malignancies, alkylating agents are the oldest class of anticancer agents. A biologic alkylating agent exerts its cytotoxic effects by forming DNA adducts and DNA interstrand crosslinks, thereby inhibiting rapidly proliferating cells. Mechlorethamine Oxide is an antineoplastic agent used to treat Hodgkin desease and Lymphoma. Known under the brand names of Mustargen and Valchlor in USA. The FDA granted marketing approval for the orphan drug Valchlor (mechlorethamine) gel on August 23, 2013 for the topical treatment of stage IA and IB mycosis fungoides-type cutaneous T-cell lymphoma (CTCL) in patients who have received prior skin-directed therapy. Each tube of Valchlor contains 0.016% of mechlorethamine which is equivalent to 0.02% mechlorethamine HCL.
Status:
Possibly Marketed Outside US
Source:
Canada:PLATINUM MURIATICUM
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Conditions:

Diamminedichlorodihydroxyplatinum IV is the platinum-based antineoplasticis agent. Oxaliplatin is cis, cis, trans- isomer of Diamminedichlorodihydroxyplatinum IV. Oxaliplatin show high stability and therefore can be utilized orally for outpatient care. Although oxoplatin is capable of binding directly to DNA after prolonged incubation, platinum(IV) agents are considered to be largely inert prodrugs that are converted to highly cytotoxic platinum(II) compounds by reducing substances, enzymes, or microenvironmental conditions. Reaction of oxoplatin with 0.1 M hydrogen chloride mimicking gastric acid yields cis-diammine-tetrachlorido-platinum(IV) (DATCP[IV]), which exhibits two-fold increased activity. The oxoplatin metabolite DATCP(IV) constitutes a potent cytotoxic derivative that may be produced by gastric acid or acidic areas prevailing in larger solid tumors, depending on the respective pharmaceutical formulation of oxoplatin.
Elliptinium is an antineoplastic agent, which was used in the treatment of metastatic breast cancer in France under the name Celiptium. The drug is known to intercalate into DNA and inhibit topoisomerase II. Several studies have demonstrated that this molecule can be oxidized, yielding a reactive electrophilic form, which is able to bind covalently to a nucleophilic biological molecule.
Status:
Possibly Marketed Outside US
Source:
NCT02088515: Phase 4 Interventional Completed Squamous Cell Carcinoma
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Nedaplatin is a second-generation cisplatin analogue with antineoplastic activity. nedaplatin forms reactive platinum complexes that bind to nucelophillic groups in DNA, resulting in intrastrand and interstrand DNA cross-links, apoptosis and cell death. It is currently registered for the treatment of various cancers (head and neck, testicular, lung, ovarian, cervical, non-small-cell lung) in Japan. The most commonly reported adverse reactions include nausea, vomiting, loss of appetite and hair loss. Nedaplatin may also cause nephrotoxicity at therapeutic doses, especially in patients with deteriorating renal function.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Satraplatin is a fourth-generation platinum-based anticancer drug developed by GPC Biotech, Inc. Unlike its predecessors cisplatin and carboplatin, which were administered intravenously, satraplatin was developed for oral administration. Satraplatin mediates its action through the formation of DNA adducts and inter- and intra-strand crosslinks. These adducts distort the DNA template with a deceleration of cells in S phase followed with G2 phase arrest. Satraplatin also inhibits DNA replication and transcription and induces signal transduction pathway, leading to cell cycle arrest and apoptosis. Satraplatin was investigated in phase III clinical trials against metastatic castrate-resistant prostate cancer. Despite the improvement in progression-free survival and palliation, overall survival was not improved with satraplatin therapy. The median survival was 61.3 weeks in the satraplatin group and 61.4 weeks in the prednisone and placebo group. In July 2007, GPC Biotech announced the withdrawal of the New Drug Application (NDA) for satraplatin, and the development of the drug was discontinued.
Status:
Possibly Marketed Outside US
Source:
DIANHYDROGALACTITOL by Vargha, L. et al.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Dianhydrogalactitol (VAL-083 or NSC-132313) a cytostatic sugar derivative, is alpha,omega-substituted hexitol acting as bifunctional alkylating agent. It induces interstrand crosslinks at N7 guanines leading to doublestrand breaks and HR activation independent of MGMT, and mediating cell cycle arrest through p53-dependent and p53-independent pathways. Dianhydrogalactitol is approved as a cancer chemotherapeutic in China for the treatment of chronic myelogenous leukemia and lung cancer. The drug has not been approved for any indication outside of China. DelMar Pharmaceuticals is developing dianhydrogalactitol for the treatment of intracranial tumors.
Status:
Possibly Marketed Outside US
Source:
SUNPLA by Sunkyong Industries
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Eptaplatin (also known as Heptaplatin) is a third-generation platinum antitumor drug, which has been approved for the clinical treatment of advanced gastric cancer in Korea. Although the anticancer mechanism of eptaplatin has not been studied well, it is supposed to be similar to that of cisplatin and oxaliplatin. Eptaplatin may bind to DNA to form various types of adducts, thus leading to cell death.
Ornidazole is nitroimidazole derivative. It is an antiprotozoal drug that has proven to be effective against Trichomonas vaginalis, Entoamoeba histolytica, Giardia lamblia and Helicobacter pylori. The reduction of the nitro group and the generation of short-lived reactive intermediates are the basis of its parasiticidal activity. Ornidazole is a DNA-tropic drug with selective activity against microorganisms with enzyme systems capable of reducing the nitrogroup and catalyze the interaction between ferrodoxin proteins and nitrocompounds. After the drug penetrates the microbial cell, the mechanism of its action is based reducing the nitrogroup under the influence of the microorganism’s nitroreductases and the activity of the reduced nitroimidazole. The reduction products create compounds with DNA causing it to degrade, and disrupt the DNA replication and transcription processes. Furthermore, the drug’s metabolism products have cytotoxic properties and disrupt cellular respiration processes. It is indicated for the treatment of anaerobic systemic infections caused by ornidazole-sensitive microflora, prevention of infections caused by anaerobic bacteria, during operative treatment (especially middle and straight intestine surgeries), gynecological surgeries, severe intestinal ameobiasis, all extra-intestinal ameobiasis forms, giardiasis. Ornidazole was shown to be effective for the prevention of recurrence of Crohn's disease after ileocolonic resection.
mixture
Status:
First approved in 2002

Class:
MIXTURE

Targets:


Oxaliplatin (brand name Eloxatin), a new generation of platinum derivatives discovered by Prof Kidani in 1976 at Nagoya University in Japan, was licensed-in and developed by Debiopharm. Eloxatin is typically administered in combination with fluorouracil and leucovorin for the adjuvant treatment of stage III colon cancer and for the treatment of advanced carcinoma of the colon or rectum. Oxaliplatin undergoes nonenzymatic conversion in physiologic solutions to active derivatives via displacement of the labile oxalate ligand. Several transient reactive species are formed, including monoaquo and diaquo 1,2-diaminocyclohexane (DACH) platinum, which covalently bind with macromolecules. Both inter- and intrastrand Pt-DNA crosslinks are formed. Crosslinks are formed between the N7 positions of two adjacent guanines (GG), adjacent adenine-guanines (AG), and guanines separated by an intervening nucleotide (GNG). These crosslinks inhibit DNA replication and transcription. Cytotoxicity is cell-cycle nonspecific.

Showing 141 - 150 of 282 results