Synonym
DJ927; DJ-927; DJ 927; Tesetaxel
IUPAC/Chemical Name
(2aS,3S,4S,6S,8aR,10R,11bR,13aR)-2a-acetoxy-6-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-3-(3-fluoropyridin-2-yl)-2-hydroxypropanoyl)oxy)-10-((dimethylamino)methyl)-4-hydroxy-7,11b,14,14-tetramethyl-2a,2b,3,4,5,6,8a,11a,11b,12,13,13a-dodecahydro-2H-4,8-methanooxeto[3'',2'':3',4']benzo[1',2':3,4]cyclodeca[1,2-d][1,3]dioxol-3-yl benzoate
InChi Key
MODVSQKJJIBWPZ-MILZTGCVSA-N
InChi Code
InChI=1S/C46H60FN3O13/c1-24-28(58-40(54)34(52)33(32-27(47)17-14-20-48-32)49-41(55)63-42(3,4)5)21-46(56)38(61-39(53)26-15-12-11-13-16-26)36-44(8,19-18-29-45(36,23-57-29)62-25(2)51)37-35(31(24)43(46,6)7)59-30(60-37)22-50(9)10/h11-17,20,28-30,33-38,52,56H,18-19,21-23H2,1-10H3,(H,49,55)/t28-,29+,30+,33-,34+,35+,36?,37?,38-,44+,45-,46+/m0/s1
SMILES Code
O=C(O[C@H]([C@]1(O)C[C@H](OC([C@H](O)[C@@H](NC(OC(C)(C)C)=O)C2=NC=CC=C2F)=O)C(C)=C3C1(C)C)C4[C@@](C5[C@]3([H])O[C@@H](CN(C)C)O5)(C)CC[C@]6([H])[C@@]4(OC(C)=O)CO6)C7=CC=CC=C7
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>5 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Tesetaxel is a novel, orally absorbed, semi-synthetic taxane that is in the same class of drugs as paclitaxel and docetaxel. However, both prototype agents suffer from serious safety issues, particularly hypersensitivity reactions related to intravenous infusions that are occasionally fatal and that require careful premedication and observation. Other prominent side-effects of this drug class include myelosuppression (low blood counts) and peripheral neuropathy (disabling nerve damage). With administration as an oral capsule, tesetaxel was developed to maintain the high antitumor activity of the taxane drug class while eliminating infusion reactions, reducing neuropathy, and increasing patient convenience. The oral route also enables development of novel schedules that may expand dosing options when tesetaxel is used alone or in combination with other anticancer drugs. Preclinically, tesetaxel has demonstrated substantially higher activity against cell lines that were resistant to paclitaxel and docetaxel, since acquired resistance is not mediated by the multidrug-resistant p-glycoprotein. As a late Phase 2 oncology product, tesetaxel has demonstrated anticancer activity in its initial clinical trials, and the drug has not been associated with the severe infusion reactions that are linked with other taxanes. Moreover, unlike other oral taxanes, nerve damage has not been a prominent side effect of tesetaxel. Thus, the drug offers substantial opportunities to improve patient convenience, safety, and anticancer activity. More than 250 patients worldwide have been treated with oral tesetaxel in Phase 1 and Phase 2 clinical trials. For more information, please visit http://www.medicalnewstoday.com/articles/132058.php.
