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Restrict the search for
uracil mustard
to a specific field?
Status:
US Approved Rx
(1957)
Source:
NDA010669
(1957)
Source URL:
First approved in 1957
Source:
NDA010669
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Chlorambucil is a bifunctional 12 alkylating agent of the nitrogen mustard type that has been found active against selected human 13 neoplastic diseases. Chlorambucil alkylates and cross-links DNA during all phases of the cell cycle, inducing DNA damage via three different methods of covalent adduct generation with double-helical DNA. Bone marrow suppression (anemia, neutropenia, thrombocytopenia) is the most commonly occurring side effect of chlorambucil. There are no known drug/drug interactions with chlorambucil.
Status:
US Approved Rx
(2013)
Source:
NDA202317
(2013)
Source URL:
First approved in 1949
Source:
MUSTARGEN by RECORDATI RARE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Mechlorethamine also known as mustine, brand name MUSTARGEN administered intravenously is the prototype anticancer chemotherapeutic drug, is indicated for the palliative treatment of Hodgkin's disease (Stages III and IV), lymphosarcoma, chronic myelocytic or chronic lymphocytic leukemia, polycythemia vera, mycosis fungoides, and bronchogenic carcinoma. In 2013 was approved orphan drug Valchlor (mechlorethamine) gel 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. Mechlorethamine belongs to the group of nitrogen mustard alkylating agents. Alkylating agents work by three different mechanisms: attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations all of which achieve the same end result - disruption of DNA function and cell death.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Mannomustine is a substance synthesized as one of a series of compounds linking the actively cytotoxic chemical group beta-chlorethylamine with a naturally
occurring substance, mannitol. Mannomustine is an alkylating agent with antineoplastic properties. It was being studied in the treatment of hematologic malignancies.
Status:
Investigational
Source:
NCT01168791: Phase 3 Interventional Completed Soft Tissue Sarcoma
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Palifosfamide or ZIO-201 (isophosphoramide mustard; IPM), a bi-functional DNA alkylator, is the active metabolite of ifosfamide (IFOS). IFOS and the related drug cyclophosphamide (CPA) are widely used anti-cancer drugs. Both are pro-drugs and need to be metabolized to be active. Their clinical use is limited by the toxicity associated with some of their metabolites. Palifosfamide has shown efficacy in diverse cancer models. ZIOPHARM Oncology Inc, under license from Dekk-Tec Inc, was developing palifosfamide, a formulation of isophosphoramide mustard with tris(hydroxymethyl)aminomethane salt-stabilization (palifosfamide-tris) and previously with lysine-stabilization (palifosfamide-lys). Preclinical studies and phase I and I/II clinical trials demonstrated that palifosfamide-tris had an antitumor efficiency comparable or superior to that of ifosfamide. To date ZIO-201 is not present in ZIOPHARM pipeline.
Status:
Investigational
Source:
INN:galamustine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Galamustine (C6-galactose mustard or C6-GLM ) is a compound that has demonstrated anti-cancer activity. Its effect on cell growth and cell cycle kinetics was studied in leukemia. Because less bone marrow toxicity was reported for this compound compared to nitrogen mustard, the development of galamustine for clinical trials in humans was considered.
Status:
Investigational
Source:
INN:oxeclosporin [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Oxeclosporin (previously known as SDZ IMM 125 and now called as tigderimus) was developed as an immunosuppressive drug. It was shown that the drug possessed apoptotic activity via induction of uptake of extracellular calcium. The increased intracellular calcium might directly cause apoptosis by increasing the caspase-3 activity. Oxeclosporin was studied in clinical trials in patients with severe psoriasis. In addition, it was used for the treatment of rheumatoid arthritis and transplant rejection. However, all these studies were discontinued. Besides, oxeclosporin is participating in phase II trials in Europe for the treatment of asthma and in Switzerland for the treatment of cancer. However, information about the further development of this drug is not available.
Status:
Investigational
Source:
NCT02073838: Phase 2 Human clinical trial Completed Leukemia, Myeloid, Acute/genetics/metabolism
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Status:
Investigational
Source:
NCT01746979: Phase 3 Interventional Completed Metastatic or Locally Advanced Unresectable Pancreatic Adenocarcinoma
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Evofosfamide, also formerly known as TH-302, is an investigational hypoxia-activated prodrug and is used to target cancerous cells under hypoxic conditions, which is a feature possessed by multiple solid tumors including glioblastoma and pancreatic cancer. Within regions of tumor hypoxia, evofosfamide releases bromo isophosphoramide mustard (Br-IPM), a potent DNA alkylating agent that kills tumor cells by forming DNA crosslinks. Once activated in hypoxic tissues, Br-IPM can also diffuse into surrounding oxygenated regions of the tumor and kill cells there via a “bystander effect”. Because of its preferential activation in the targeted hypoxic regions of solid tumors, evofosfamide may be less likely to produce broad systemic toxicity seen with untargeted cytotoxic chemotherapies.
Status:
Investigational
Source:
NCT01677338: Phase 2 Interventional Completed Dyspeptic Subjects
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Otsuka Pharmaceutical was developing URACIL C-13, 2- ([2-13C]uracil) breath test for diagnosis of cancer and gastric emptying disorders. Dihydropyrimidine dehydrogenase (DPD) deficiency is critical in the predisposition to 5-fluorouracil dose-related toxicity. The phenotypic [2-(13)C]uracil breath test (UraBT) demonstrated 96% specificity and 100% sensitivity for identification of DPD deficiency. Phase II development of the breath test was ongoing. As phase II clinical study didn't exploit performance as diagnostic medicines, the development of [2-13C]uracil was discontinued.
Status:
Investigational
Source:
Przegl Dermatol. 1981;68(1):95-9.: Not Applicable Human clinical trial Completed Scalp Dermatoses
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
