Soblidotin
DRACPC ID DRACPC0057
Active Ingredients Soblidotin
Description A tetrapeptide derivative of dolastatin 10. Soblidotin inhibits tubulin polymerization, resulting in cell cycle arrest and induction of apoptosis. It has a role as a microtubule-destabilising agent, an antineoplastic agent and an apoptosis inducer. It is functionally related to a 2-phenylethylamine and a L-valine.
Synonyms Auristatin PE; TZT-1027; N(2)-(N,N-Dimethyl-valyl)-N-(2-methoxy-4-(2-(1-methoxy-2-methyl-3-oxo-3-((2-phenylethyl)amino)propyl)-1-pyrrolidinyl)-1-(1-methylpropyl)-4-oxobutyl)-N-methyl-valinamide; Soblidotin
Type Small Molecule
Disease Sarcoma, Lung Cancer
Classification
Tubulin inhibitor Peptide and derivative
Structure Information
Molecular Formula C39H67N5O6
Molecular Weight 702
Active Sequence Not available
Sequence Length Not available
Modification Not available
IUPAC Name (2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-(2-phenylethylamino)propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide
InChI InChI=1S/C39H67N5O6/c1-13-27(6)35(43(10)39(48)33(25(2)3)41-38(47)34(26(4)5)42(8)9)31(49-11)24-32(45)44-23-17-20-30(44)36(50-12)28(7)37(46)40-22-21-29-18-15-14-16-19-29/h14-16,18-19,25-28,30-31,33-36H,13,17,20-24H2,1-12H3,(H,40,46)(H,41,47)/t27-,28+,30-,31+,33-,34-,35-,36+/m0/s1
InChI_Key DZMVCVHATYROOS-ZBFGKEHZSA-N
SMILES [H][C@@]1([C@@H]([C@H](C(NCCC2=CC=CC=C2)=O)C)OC)CCCN1C(C[C@H]([C@@H](N(C([C@H](C(C)C)NC([C@@H](N(C)C)C(C)C)=O)=O)C)[C@H](CC)C)OC)=O
External Codes
PubChem CID 6918315
DrugBank Accession Number DB12677
NCI Thesaurus Code C26672
UNII DQC51A0WQH GSRS
CAS 149606-27-9
Drug approval
Drug indication
Soblidotin has been used in trials studying the treatment of Sarcoma, Lung Cancer, and Unspecified Adult Solid Tumor.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT00064220 | A Phase II Study of Intravenous TZT-1027, Administered Weekly Times Two, Every Three Weeks, to Patients With Advanced or Metastatic Soft Tissue Sarcomas (STS) With Prior Exposure to Anthracycline-Based Chemotherapy | Sarcoma | Phase 2 | Treatment |
| NCT00061854 | A Phase II Study Of Intravenous TZT-1027, Administered Weekly Times Two, Every Three Weeks, To Patients With Progressive Locally Advanced Or Metastatic Non-Small Cell Lung Cancer (NSCLC) Following Treatment With Platinum-Based Chemotherapy | Lung Cancer | Phase 2 | Treatment |
| NCT00072228 | Phase I Study of Soblidotin and Gemcitabine in Patients With Locally Advanced or Metastatic Solid Tumors | Unspecified Adult Solid Tumor, Protocol Specific | Phase 1 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
