Talabostat

DCTPepD ID  DCTPepD0046

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

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

Structure

 

Show IUPAC/InChI/SMILES

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.





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