Plocabulin
DRACPC ID DRACPC0093
Active Ingredients Plocabulin
Description A marine-derived, synthetically produced compound with potential antineoplastic activity. Plocabulin covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death.
Synonyms PM-060184; PM060184; Plocabulin
Type Small Molecule
Disease Solid Tumors, Advanced Colorectal Cancer
Classification
Microtubule inhibitor Peptide and derivative
Structure Information
Molecular Formula C31H45N3O7
Molecular Weight 571.7
Active Sequence Not available
Sequence Length Not available
Modification Not available
IUPAC Name [(1Z,4S,6Z)-1-[[(2S)-2-[[(2Z,4Z,6E,8S)-8-[(2S)-5-methoxy-6-oxo-2,3-dihydropyran-2-yl]-6-methylnona-2,4,6-trienoyl]amino]-3,3-dimethylbutanoyl]amino]octa-1,6-dien-4-yl] carbamate
InChI InChI=1S/C31H45N3O7/c1-8-9-14-23(40-30(32)38)15-12-19-33-28(36)27(31(4,5)6)34-26(35)16-11-10-13-21(2)20-22(3)24-17-18-25(39-7)29(37)41-24/h8-13,16,18-20,22-24,27H,14-15,17H2,1-7H3,(H2,32,38)(H,33,36)(H,34,35)/b9-8-,13-10-,16-11-,19-12-,21-20+/t22-,23-,24-,27+/m0/s1
InChI_Key IEKGSKLKBICCHQ-BDOJOPHNSA-N
SMILES C/C=C\C[C@H](OC(N)=O)C/C=C\NC([C@H](C(C)(C)C)NC(/C=C\C=C/C(C)=C/[C@@H]([C@@H]1CC=C(C(O1)=O)OC)C)=O)=O
External Codes
PubChem CID 57788271
DrugBank Accession Number Not available
NCI Thesaurus Code C95888
UNII 52Y8L60CR7 GSRS
CAS 960210-99-5
Drug approval
Drug indication
Investigated for use/treatment in Solid Tumors, Advanced Colorectal Cancer.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT01299636 | Phase I, Multicenter, Open-label, Dose-escalating, Clinical and Pharmacokinetic Study of PM060184 Administered Intravenously to Patients With Advanced Solid Tumors | Solid Tumors | Phase 1 | Treatment |
| NCT03427268 | A Phase II, Open-label, Multicentre Study of PM060184 in Patients With Advanced Colorectal Cancer After Standard Treatment. | Advanced Colorectal Cancer | Phase 2 | Treatment |
| NCT02533674 | Phase I Multicenter, Open-label, Clinical and Pharmacokinetic Study of PM060184 in Combination With Gemcitabine in Selected Patients With Advanced Solid Tumors | Solid Tumors | Phase 1 | Other |
More clinical information is obtained from ClinicalTrials.gov.
