Valspodar
DRACPC ID DRACPC0087
Active Ingredients Valspodar
Description An analogue of cyclosporin-A. Valspodar inhibits p-glycoprotein, the multidrug resistance efflux pump, thereby restoring the retention and activity of some drugs in some drug-resistant tumor cells. This agent also induces caspase-mediated apoptosis
Synonyms 6-[(2S,4R,6E)-4-Methyl-2-(methylamino)-3-oxo-6-octenoic Acid]cyclosporin D; Amdray; Cyclo((2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoyl)-L-valyl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl-L-alanyl-D-alanyl-N-me; PSC-833; PSC833; SZD PSC 833; Valspodar; VP16
Type Small Molecule
Disease Sarcoma, Leukemia, Lymphoma, Breast Cancer
Classification
Peptide and derivative Cyclic
Structure Information
Molecular Formula C63H111N11O12
Molecular Weight 1214.6
Active Sequence Not available
Sequence Length Not available
Modification Not available
IUPAC Name (3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-1,4,7,10,12,15,19,25,28-nonamethyl-33-[(E,2R)-2-methylhex-4-enoyl]-6,9,18,24-tetrakis(2-methylpropyl)-3,21,30-tri(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone
InChI InChI=1S/C63H111N11O12/c1-26-27-28-41(16)53(76)52-57(80)67-49(38(10)11)61(84)68(19)33-48(75)69(20)44(29-34(2)3)56(79)66-50(39(12)13)62(85)70(21)45(30-35(4)5)55(78)64-42(17)54(77)65-43(18)58(81)71(22)46(31-36(6)7)59(82)72(23)47(32-37(8)9)60(83)73(24)51(40(14)15)63(86)74(52)25/h26-27,34-47,49-52H,28-33H2,1-25H3,(H,64,78)(H,65,77)(H,66,79)(H,67,80)/b27-26+/t41-,42+,43-,44+,45+,46+,47+,49+,50+,51+,52+/m1/s1
InChI_Key YJDYDFNKCBANTM-QCWCSKBGSA-N
SMILES O=C([C@H](C(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@@H](C)NC([C@H](C)NC([C@H](CC(C)C)N(C)C([C@H](C(C)C)NC([C@H](CC(C)C)N(C)C(CN(C)C([C@H](C(C)C)N1)=O)=O)=O)=O)=O)=O)=O)=O)=O)N(C)[C@@H](C([C@H](C)C/C=C/C)=O)C1=O
External Codes
PubChem CID 5281884
DrugBank Accession Number DB11869
NCI Thesaurus Code C1405
UNII Q7ZP55KF3X GSRS
CAS 121584-18-7
Drug approval
Drug indication
Valspodar has been used in trials studying the treatment of Cancer, Sarcoma, Leukemia, Lymphoma, and Breast Cancer, among others.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT00003207 | Phase I Study on Doxil and SDZ PSC 833 in the Treatment of AIDS-Associated Kaposi's Sarcoma and Other Advanced Malignancies | Sarcoma; Unspecified Adult Solid Tumor, Protocol Specific | Phase 1 | Treatment |
| NCT00002912 | A PHASE I COOPERATIVE AGREEMENT PEDIATRIC TRIAL OF MITOXANTRONE, ETOPOSIDE AND PSC-833 (PSC-ME) THERAPY IN PATIENTS WITH RELAPSED AND REFRACTORY ACUTE LEUKEMIA | Leukemia | Phase 1 | Treatment |
| NCT00001302 | A Phase I Study of Infusional Chemotherapy With the P-Glycoprotein Antagonist PSC 833 | Breast Cancer; Kidney Neoplasm; Lymphoma; Neoplasm Metastasis; Ovarian Cancer | Phase 1 | Treatment |
| NCT00002937 | A Phase II Randomized Study of Paclitaxel Versus Paclitaxel + PSC833 for Advanced Breast Cancer (Recurring Less Than 6 Months Since Adjuvant or as Second Line for Advanced Disease | Breast Cancer | Phase 2 | Treatment |
| NCT00002878 | A PHASE III STUDY OF PSC-833 IN COMBINATION WITH VINCRISTINE, DOXORUBICIN AND DEXAMETHASONE (PSC-833/VAD) VERSUS VAD ALONE IN PATIENTS WITH RELAPSING OR REFRACTORY MULTIPLE MYELOMA | Multiple Myeloma and Plasma Cell Neoplasm | Phase 3 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
