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Details

Stereochemistry ACHIRAL
Molecular Formula C24H30ClN7O2S
Molecular Weight 516.0606
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DUBERMATINIB

SMILES

CN(C)S(=O)(=O)c1ccccc1N=c2c(cnc(Nc3ccc(cc3)CN4CCN(C)CC4)[nH]2)Cl

InChI

InChIKey=YUAALFPUEOYPNX-UHFFFAOYSA-N
InChI=1S/C24H30ClN7O2S/c1-30(2)35(33,34)22-7-5-4-6-21(22)28-23-20(25)16-26-24(29-23)27-19-10-8-18(9-11-19)17-32-14-12-31(3)13-15-32/h4-11,16H,12-15,17H2,1-3H3,(H2,26,27,28,29)

HIDE SMILES / InChI

Molecular Formula C24H30ClN7O2S
Molecular Weight 516.0606
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

HCI-2084 (wider known as TP-0903) is developing by Tolero Pharmaceuticals for the treatment of different cancers. HCI-2084 is a small molecule AXL receptor tyrosine kinase (RTK) inhibitor. AXL is involved in maintaining a mesenchymal phenotype in cancer cells that enhanced cell survival in stressed environments, and increased resistance to targeted therapies compared to epithelial cells. AXL overexpression has been observed in multiple tumor types that have acquired resistance to various agents. TP-0903 is participating in phase I/II clinical trial in patients with previously treated chronic lymphocytic leukemia (CLL). This study will investigate the safety, pharmacokinetics, pharmacodynamics, and clinical activity of TP-0903. Besides, phase I is currently being conducted in patients with advanced solid tumors in the presence of TP-0903. In addition, TP-0903 was investigated in neuroblastoma (NB) cells, where this drug makes NB cells more vulnerable to the conventional chemotherapeutics.

Approval Year

PubMed

PubMed

TitleDatePubMed
Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.
2011 Dec 8
Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors.
2015 May 1
Chronic lymphocytic leukemia cells from ibrutinib treated patients are sensitive to Axl receptor tyrosine kinase inhibitor therapy.
2018 Dec 14
TP-0903 inhibits neuroblastoma cell growth and enhances the sensitivity to conventional chemotherapy.
2018 Jan 5

Sample Use Guides

Monotherapy: PHASE 1: TP-0903 (HCI-2084) will be a 25 mg flat dose. The study drug will be administered orally once daily for 28 days (each cycle is 28 days; no drug-free period). Patients may continue to receive TP-0903 in 28-day cycles at the same dose given during Cycle 1 until they experience unacceptable toxicity or unequivocal disease progression. No intrapatient escalation of the TP-0903 dose is permitted. PHASE 2: The starting dose of TP-0903 will be the RP2D determined during Phase 1. TP 0903 will be administered orally at a fixed dose once daily for 28 days (each cycle is 28 days; no drug-free period) with repeated cycles permitted until a patient experiences unacceptable toxicity or unequivocal disease progression.
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Fri Jun 25 23:12:27 UTC 2021
Edited
by admin
on Fri Jun 25 23:12:27 UTC 2021
Record UNII
14D65TV20J
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DUBERMATINIB
INN   USAN  
Official Name English
TP0903
Code English
DUBERMATINIB [INN]
Common Name English
BENZENESULFONAMIDE, 2-((5-CHLORO-2-((4-((4-METHYL-1-PIPERAZINYL)METHYL)PHENYL)AMINO)-4-PYRIMIDINYL)AMINO)-N,N-DIMETHYL-
Common Name English
DUBERMATINIB [WHO-DD]
Common Name English
DUBERMATINIB [USAN]
USAN  
Common Name English
TP-0903
Code English
35-CHLORO-N,N,74-TRIMETHYL-2,4-DIAZA-3(4,2)-PYRIMIDINA-7(1)-PIPERAZINA-1(1),5(1,4)-DIBENZENAHEPTAPHANE-12-SULFONAMIDE
Systematic Name English
Code System Code Type Description
FDA UNII
14D65TV20J
Created by admin on Fri Jun 25 23:12:27 UTC 2021 , Edited by admin on Fri Jun 25 23:12:27 UTC 2021
PRIMARY
INN
10925
Created by admin on Fri Jun 25 23:12:27 UTC 2021 , Edited by admin on Fri Jun 25 23:12:27 UTC 2021
PRIMARY
CAS
1341200-45-0
Created by admin on Fri Jun 25 23:12:27 UTC 2021 , Edited by admin on Fri Jun 25 23:12:27 UTC 2021
PRIMARY
DRUG BANK
DB15187
Created by admin on Fri Jun 25 23:12:27 UTC 2021 , Edited by admin on Fri Jun 25 23:12:27 UTC 2021
PRIMARY
PUBCHEM
56839178
Created by admin on Fri Jun 25 23:12:27 UTC 2021 , Edited by admin on Fri Jun 25 23:12:27 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Related Record Type Details
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