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Restrict the search for
uracil mustard
to a specific field?
Status:
US Approved Rx
(1998)
Source:
ANDA040278
(1998)
Source URL:
First approved in 1962
Source:
FLUOROURACIL by SPECTRUM PHARMS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Fluorouracil is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances from becoming incorporated into DNA during the "S" phase (of the cell cycle), stopping normal development and division. Fluorouracil blocks an enzyme which converts the cytosine nucleotide into the deoxy derivative. In addition, DNA synthesis is further inhibited because Fluorouracil blocks the incorporation of the thymidine nucleotide into the DNA strand. Fluorouracil is used for the topical treatment of multiple actinic or solar keratoses. In the 5% strength it is also useful in the treatment of superficial basal cell carcinomas when conventional methods are impractical, such as with multiple lesions or difficult treatment sites. Fluorouracil injection is indicated in the palliative management of some types of cancer, including colon, esophageal, gastric, rectum, breast, biliary tract, stomach, head and neck, cervical, pancreas, renal cell, and carcinoid.
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:
INN:palifosfamide [INN]
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:
NCT02073838: Phase 2 Human clinical trial Completed Leukemia, Myeloid, Acute/genetics/metabolism
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Status:
Investigational
Source:
JAN:EVOFOSFAMIDE [JAN]
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:
JAN:URACIL (2-13C) [JAN]
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)
Class (Stereo):
CHEMICAL (RACEMIC)
Perfosfamide is the active metabolite of the nitrogen mustard cyclophosphamide with potent antineoplastic and immunosuppressive properties. Perfosfamide alkylates DNA, thereby inhibiting DNA replication and RNA and protein synthesis. The incubation of normal human marrow cells with perfosfamide has a toxic effect on granulocyte-macrophage progenitor cells that is dose as well as white blood cell concentration dependent. It is likely that this dependency of the perfosfamide stem cell effect is caused not only by the target white blood cell concentration but by the suspension’s total protein concentration. Autologous bone marrow transplantation with perfosfamide purging in patients with acute myeloid leukemia in second complete remission produced results similar to that reported with allogeneic bone marrow transplantation. Perfosfamide had been in phase III clinical trial for the treatment of acute myeloid leukemia. However, this development was discontinued.
