Talabostat
DRACPC ID DRACPC0046
Active Ingredients Talabostat
Description A small molecule with antineoplastic and hematopoiesis- stimulating activities. By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, talabostat inhibits dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity. This agent may also stimulate the production of colony stimulating factors, such as granulocyte colony stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis. Dipeptidyl peptidases are involved in the activation of polypeptide hormones and chemokines.
Synonyms [(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid; BXCL 701; BXCL-701; PT-100; Talabostat
Type Small Molecule
Disease Lymphoma, Lung cancer, Melanoma, Pancreatic cancer, Brain cancer
Classification
Dipeptidyl peptidases inhibitor Amino acid and derivative
Structure Information
Molecular Formula C9H19BN2O3
Molecular Weight 214.07
Active Sequence Not available
Sequence Length Not available
Modification Not available
IUPAC Name [(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid
InChI InChI=1S/C9H19BN2O3/c1-6(2)8(11)9(13)12-5-3-4-7(12)10(14)15/h6-8,14-15H,3-5,11H2,1-2H3/t7-,8-/m0/s1
InChI_Key FKCMADOPPWWGNZ-YUMQZZPRSA-N
SMILES CC(C)[C@H](N)C(N1[C@H](B(O)O)CCC1)=O
External Codes
PubChem CID 6918572
DrugBank Accession Number DB06182
NCI Thesaurus Code C48264
UNII KZ1O2SH88Z GSRS
CAS 149682-77-9
Drug approval
Drug indication
Investigated for use/treatment in lymphoma (non-hodgkin's), leukemia (lymphoid), lung cancer, melanoma, and pancreatic cancer.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT00080080 | Phase 2 Study of Talabostat and Docetaxel in Advanced Non-Small Cell Lung Cancer | Lung Cancer | Phase 2 | Treatment |
| NCT04171219 | A Phase 2 Basket Study of BXCL701, a Small Molecule Inhibitor of Dipeptidyl Peptidases (DPP), Administered in Combination With Pembrolizumab in Patients With Advanced Solid Cancers | Advanced Malignant Solid Neoplasm; Recurrent Malignant Solid Neoplasm | Phase 2 | Treatment |
| NCT00489710 | A Phase II Study of Talabostat in Patients With Metastatic Renal Cell Carcinoma | Kidney Cancer | Phase 2 | Treatment |
| NCT04123574 | A Pilot Proof of Mechanism Study of BXCL701, a Small Molecule Inhibitor of Dipeptidyl Peptidases (DPPs), in Patients With Pancreatic Cancer | Cancer of Pancreas; Cancer of the Pancreas; Neoplasms, Pancreatic; Pancreas Cancer; Pancreatic Cancer | Early Phase 1 | Treatment |
| NCT00290017 | A Phase 3, Randomized, Double-Blind, Multicenter Study of Talabostat and Pemetrexed vs. Pemetrexed and Placebo in Patients With Advanced (Stage IIIB/IV) Non-Small Cell Lung Cancer (NSCLC) After Failure of Platinum-Based Chemotherapy | Carcinoma, Non-Small-Cell Lung; Lung Cancer; Neoplasms, Lung; Neoplasms, Pulmonary | Phase 3 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
