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Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
10-deactyltaxol (10-deacetylpaclitaxel) is a naturally occurring taxane related to taxol (paclitaxel). Taxol is an antitumor drug with cytotoxic properties that correlate with its microtubule-stabilizing activities. When compared to paclitaxel 10-deacetyltaxol is 100% as active as paclitaxel in promoting in vitro microtubule assembly, but is only 30% as cytotoxic as paclitaxel. 10-deactyltaxol is a semi-synthetic precursor of paclitaxel and considered to be paclitaxel impurity. 10-deactyltaxol, isolated from the bark of Taxus brevifolia, was converted into paclitaxel in one composite step (trimethylsilylation, acetylation, and desilylation) and in an overall yield of 80-85%.
(Z)-β-Santalol is a key component of sandalwood oil, which when purified, can be used to treat the common cold, bronchitis, fever, and urinary tract infections, and it has also been shown to have anti-inflammatory properties and cause autophagy in proliferating keratinocytes. β-Santalol has antiviral and anticancer activities. As of 2002, about 60 tons of sandalwood oil are produced annually by steam distillation of the heartwood of Santalum album.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Mertansine (Maytansine) is a 19–member ansa macrolide structure attached to a chlorinated benzenering. It was originally isolated from the shrub Maytenus ovatus. Mertansine (DM1) is a tubulin inhibitor, it inhibits the assembly of microtubules by binding to tubulin, with a linker structure can create an antibody-drug conjugate (ADC). Mertansine is a potent microtubule-targeted compound that induces mitotic arrest and kills tumor cells at sub-nanomolar concentrations. The antimitotic effect of maytansine has been attributed to its ability to inhibit microtubule assembly by binding to tubulin with a KD of ~ 1 umol/L, at or near the vinblastine-binding site. Experimental ADCs with the SPP-DM1 design include lorvotuzumab mertansine. DM1 can also be linked to an antibody using the SMCC (4-(3-mercapto-2,5-dioxo-1-pyrrolidinylmethyl)-cylohexanecarboxylic acid) linker, in which case the International Nonproprietary Name of the conjugate formed contains the word emtansine. DM1 and its attachment via these linkers result from ImmunoGen Inc research. Trastuzumab emtansine (T-DM1) is an anti-HER2/neu antibody-drug conjugate.
Status:
US Previously Marketed
Source:
MINTEZOL by MERCK SHARP DOHME
(1967)
Source URL:
First approved in 1967
Source:
MINTEZOL by MERCK SHARP DOHME
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Thiabendazole (TBZ, trade names Mintezol, Tresaderm, and Arbotect) was first introduced in 1962. This drug is a fungicide and parasiticide and is indicated for the treatment of: strongyloidiasis (threadworm), cutaneous larva migrans (creeping eruption), visceral larva migrans, trichinosis: relief of symptoms and fever and a reduction of eosinophilia have followed the use of this drug during the invasion stage of the disease. But usage of this drug was discontinued. The precise mode of action of thiabendazole on the parasite is unknown, but it may inhibit the helminthspecific enzyme fumarate reductase. It was shown, also that thiabendazole reversibly disassembles newly established blood vessels, marking it as vascular disrupting agent (VDA) and thus as a potential complementary therapeutic for use in combination with current anti-angiogenic therapies. Was shown, that vascular disruption by TBZ results from reduced tubulin levels and hyper-active Rho signaling. In addition, was confirmed, that thiabendazole slowed tumor growth and decreased vascular density in preclinical fibrosarcoma xenografts and thus, it could lead directly to the identification of a potential new therapeutic application for an inexpensive drug that is already approved for clinical use in humans.
Status:
Possibly Marketed Outside US
Source:
MUTIAN Xraphconn by Nantong MUTIAN Biotechnology Co., Ltd
(2019)
Source URL:
First approved in 2019
Source:
MUTIAN Xraphconn by Nantong MUTIAN Biotechnology Co., Ltd
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Crocin is the chemical constituent isolated from the Saffron, the dried trifid stigma of the plant Crocus sativus L. and also from the fruits of Gardenia(Gardenia jasminoides Ellis) Of the carotenoids present in saffron, highly water-soluble crocin (mono and diglycosyl esters of a polyene dicarboxylic acid, named crocetin) is responsible for the majority of its color, and appears to possess various health-promoting properties, as an antioxidant, antitumor, memory enhancer, antidepressant, anxiolytic and aphrodisiac. It is also worth noting that the crocin principle of saffron exhibited high efficacy along with no major toxicity in experimental models. A proteomic study revealed that crocin physically binds to a wide range of cellular proteins such as structural proteins, membrane transporters, and enzymes involved in ATP and redox homeostasis and signal transduction. CROCIN RICH products provide highly purified natural crocin as dietary supplements, they are the purest and most effective formulation of crocin available.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Vinflunine (Javlor) is the first fluorinated microtubule inhibitor belonging to the Vinca alkaloids family. Vinflunine, at the lowest effective concentrations, interacts with the Vinca alkaloid binding site on tubulin, suppresses microtubule dynamics (switching at microtubule ends between phases of slow growth and rapid shortening) and microtubule treadmilling (growth at the plus end and shortening at the minus end of the microtubule), causes cell cycle arrest which appears on fluorescence-activated cell sorting analysis as a G2 + M phase arrest, and is associated with an accumulation of cells in mitosis leading to cell death via apoptosis. Vinflunine has been been approved for advanced or metastatic
transitional cell carcinoma of the urothelial tract. Pierre Fabre submitted an extension to the EU authorisation to add treatment of advanced breast cancer.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Demecolcine, also called Colcemid, was isolated from the autumn crocus in 1950 and commercialized by Ciba. Initially, it was explored as a cancer drug due to its low toxicity. Demecolcine depolymerizes microtubules and limits microtubule formation (inactivates spindle fiber formation), thus arresting cells in metaphase and allowing cell harvest and karyotyping to be performed. Today, it is only used as a research tool mainly to overcome limitations of colchicine due to its very slow association and dissociation rate constants. It binds to tubulin at the same site as colchicine, but ~10-fold faster, and it also dissociates faster. Demecolcine main use has been to arrest cells in mitosis for cytogenetic analysis, though to our knowledge it offers no special advantages over other drugs in this application.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Apramycin is a broad-spectrum aminocyclitol antibiotic produced by a strain of Streptomyces tenebrarius. It has a bactericidal action against many gram-negative bacteria. Apramycin is a structurally unique antibiotic that contains a bicyclic sugar moiety and a monosubstituted deoxystreptamine. It is not approved for use in humans. Apramycin is registered for use in more than twenty countries in cattle, pigs and chickens. The drug exerts its antibacterial effect by inhibiting
protein synthesis at the level of peptidyl translocation. It is mostly used for treating gastrointestinal
infections. Apramycin is available in soluble powder and feed premix formulations.
Status:
US Approved Rx
(2017)
Source:
ANDA207563
(2017)
Source URL:
First approved in 1996
Source:
NDA020449
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Docetaxel was protected by patents (U.S. patent and European patent) which were owned by Sanofi-Aventis, and so was available only under the Taxotere brand name internationally. The European patent expired in 2010. Docetaxel is a clinically well-established anti-mitotic chemotherapy medication used for the treatment of patients with locally advanced or metastatic breast cancer after failure of prior chemotherapy. Also used as a single agent in the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of prior platinum-based chemotherapy. It is also used in combination with prednisone, in the treatment of patients with androgen independent (hormone refractory) metastatic prostate cancer. Furthermore, docetaxel has uses in the treatment of gastric adenocarcinoma and head and neck cancer. Docetaxel interferes with the normal function of microtubule growth. Whereas drugs like colchicine cause the depolymerization of microtubules in vivo, docetaxel arrests their function by having the opposite effect; it hyper-stabilizes their structure. This destroys the cell's ability to use its cytoskeleton in a flexible manner. Specifically, docetaxel binds to the β-subunit of tubulin. Tubulin is the "building block" of mictotubules, and the binding of docetaxel locks these building blocks in place. The resulting microtubule/docetaxel complex does not have the ability to disassemble. This adversely affects cell function because the shortening and lengthening of microtubules (termed dynamic instability) is necessary for their function as a transportation highway for the cell. Chromosomes, for example, rely upon this property of microtubules during mitosis. Further research has indicated that docetaxel induces programmed cell death (apoptosis) in cancer cells by binding to an apoptosis stopping protein called Bcl-2 (B-cell leukemia 2) and thus arresting its function.
Status:
US Approved Rx
(2017)
Source:
ANDA207563
(2017)
Source URL:
First approved in 1996
Source:
NDA020449
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Docetaxel was protected by patents (U.S. patent and European patent) which were owned by Sanofi-Aventis, and so was available only under the Taxotere brand name internationally. The European patent expired in 2010. Docetaxel is a clinically well-established anti-mitotic chemotherapy medication used for the treatment of patients with locally advanced or metastatic breast cancer after failure of prior chemotherapy. Also used as a single agent in the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of prior platinum-based chemotherapy. It is also used in combination with prednisone, in the treatment of patients with androgen independent (hormone refractory) metastatic prostate cancer. Furthermore, docetaxel has uses in the treatment of gastric adenocarcinoma and head and neck cancer. Docetaxel interferes with the normal function of microtubule growth. Whereas drugs like colchicine cause the depolymerization of microtubules in vivo, docetaxel arrests their function by having the opposite effect; it hyper-stabilizes their structure. This destroys the cell's ability to use its cytoskeleton in a flexible manner. Specifically, docetaxel binds to the β-subunit of tubulin. Tubulin is the "building block" of mictotubules, and the binding of docetaxel locks these building blocks in place. The resulting microtubule/docetaxel complex does not have the ability to disassemble. This adversely affects cell function because the shortening and lengthening of microtubules (termed dynamic instability) is necessary for their function as a transportation highway for the cell. Chromosomes, for example, rely upon this property of microtubules during mitosis. Further research has indicated that docetaxel induces programmed cell death (apoptosis) in cancer cells by binding to an apoptosis stopping protein called Bcl-2 (B-cell leukemia 2) and thus arresting its function.