Tesetaxel

Tesetaxel
Clinical data

ATC code	none
Legal status
Legal status	Investigational
Identifiers
IUPAC name (2aS,2bR,3S,4S,6S,8aR,10S,11aS,11bR,13aR)-2a-(acetyloxy)-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-methano[1,3]dioxolo[3,4]cyclodeca[1,2-d][1]benzoxet-3-yl benzoate
CAS Number	333754-36-2^Y
PubChem CID	6918574
ChemSpider	5293771^N
UNII	UG97LO5M8Y
Chemical and physical data
Formula	C₄₆H₆₀FN₃O₁₃
Molar mass	881.98 g/mol
3D model (JSmol)	Interactive image
SMILES CC1=C2[C@@H]3[C@H]([C@@]4(CC[C@@H]5[C@]([C@H]4[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](C6=C(C=CC=N6)F)NC(=O)OC(C)(C)C)O)O)OC(=O)C7=CC=CC=C7)(CO5)OC(=O)C)C)O[C@@H](O3)CN(C)C
InChI 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^N Key:MODVSQKJJIBWPZ-VLLPJHQWSA-N^N
^NY (what is this?) (verify)

Tesetaxel (DJ-927) is a drug being investigated for chemotherapy of various types of cancer, including breast cancer,^[1] gastric cancer,^[2] and other solid tumours.^[3]

References

↑ Clinical trial number NCT01609127 for "Tesetaxel Every 3 Weeks vs Weekly vs Capecitabine as 1st-line Therapy for Locally Advanced or Metastatic Breast Cancer" at ClinicalTrials.gov
↑ Clinical trial number NCT01348009 for "Tesetaxel Plus Capecitabine and Cisplatin in Advanced Gastric Cancer" at ClinicalTrials.gov
↑ Saif, M. W.; Sarantopoulos, J.; Patnaik, A.; Tolcher, A. W.; Takimoto, C.; Beeram, M. (2011). "Tesetaxel, a new oral taxane, in combination with capecitabine: A phase I, dose-escalation study in patients with advanced solid tumors". Cancer Chemotherapy and Pharmacology. 68 (6): 1565–1573. PMID 21547572. doi:10.1007/s00280-011-1639-3.

Block microtubule assembly	Vinca alkaloids (Vinblastine^# Vincristine^# Vinflunine^§ Vindesine Vinorelbine)
Block microtubule disassembly	Taxanes (Cabazitaxel Docetaxel^# Larotaxel Ortataxel^† Paclitaxel^# Tesetaxel) Epothilones (Ixabepilone)

Folic acid	Dihydrofolate reductase inhibitor (Aminopterin Methotrexate^# Pemetrexed Pralatrexate) Thymidylate synthase inhibitor (Raltitrexed Pemetrexed)
Purine	Adenosine deaminase inhibitor (Pentostatin) Halogenated/ribonucleotide reductase inhibitors (Cladribine Clofarabine Fludarabine) Nelarabine Thiopurine (Thioguanine^# Mercaptopurine^#)
Pyrimidine	Thymidylate synthase inhibitor (Fluorouracil^# Capecitabine Doxifluridine Tegafur (+gimeracil/oteracil) Carmofur Floxuridine) DNA polymerase inhibitor (Cytarabine^#) Ribonucleotide reductase inhibitor (Gemcitabine) Hypomethylating agent (Azacitidine Decitabine)
Deoxyribonucleotide	Ribonucleotide reductase inhibitor (Hydroxycarbamide)

I	Camptotheca (Camptothecin Cositecan^† Belotecan Gimatecan Exatecan Irinotecan Lurtotecan^‡ Silatecan^§ Topotecan Rubitecan^‡)
II	Podophyllum (Etoposide^# Teniposide)
II+Intercalation	Anthracyclines (Aclarubicin Daunorubicin^# Doxorubicin^# Epirubicin Idarubicin Amrubicin^† Pirarubicin Valrubicin Zorubicin) Anthracenediones (Mitoxantrone Pixantrone)

Alkylating	Nitrogen mustards: Mechlorethamine Cyclophosphamide^# (Ifosfamide Trofosfamide) Chlorambucil^# (Melphalan Prednimustine) Bendamustine Uramustine Estramustine phosphate Nitrosoureas: Carmustine Lomustine (Semustine) Fotemustine Nimustine Ranimustine Streptozocin Alkyl sulfonates: Busulfan (Mannosulfan Treosulfan) Aziridines: Carboquone ThioTEPA Triaziquone Triethylenemelamine
Platinum-based	Carboplatin Cisplatin Dicycloplatin Nedaplatin Oxaliplatin Satraplatin
Nonclassical	Hydrazines (Procarbazine^#) Triazenes (Dacarbazine^# Temozolomide) Altretamine Mitobronitol Pipobroman
Intercalation	Streptomyces (Actinomycin^# Bleomycin^# Mitomycins Plicamycin)

Other

Enzyme inhibitors	FI (Tipifarnib^§) CDK inhibitors (Alvocidib^† Palbociclib Ribociclib Seliciclib^†) PrI Bortezomib Carfilzomib Ixazomib PhI (Anagrelide) IMPDI (Tiazofurin^§) LI (Masoprocol) PARP inhibitor (Niraparib Olaparib Rucaparib) HDAC (Belinostat Panobinostat Romidepsin Vorinostat) PIKI (Idelalisib)
Receptor antagonists	ERA (Atrasentan) Retinoid X receptor (Bexarotene) Sex steroid (Testolactone)
Other/ungrouped	Amsacrine Trabectedin Retinoids (Alitretinoin Tretinoin) Arsenic trioxide Asparagine depleters (Asparaginase^#/Pegaspargase) Celecoxib Demecolcine Elesclomol^§ Elsamitrucin Etoglucid Lonidamine Lucanthone Mitoguazone Mitotane Oblimersen^† Omacetaxine mepesuccinate Eribulin

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