Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C27H27N9O6 |
Molecular Weight | 573.56 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NC(N)=C2N=C(CNC3=CC=C(C=C3)C(=O)N[C@@H](CCCNC(=O)C4=C(C=CC=C4)C(O)=O)C(O)=O)C=NC2=N1
InChI
InChIKey=NYQPLPNEESYGNO-IBGZPJMESA-N
InChI=1S/C27H27N9O6/c28-21-20-22(36-27(29)35-21)32-13-16(33-20)12-31-15-9-7-14(8-10-15)23(37)34-19(26(41)42)6-3-11-30-24(38)17-4-1-2-5-18(17)25(39)40/h1-2,4-5,7-10,13,19,31H,3,6,11-12H2,(H,30,38)(H,34,37)(H,39,40)(H,41,42)(H4,28,29,32,35,36)/t19-/m0/s1
Talotrexin (also known as PT-523) was developed as a nonpolyglutamatable antifolate drug for the treatment of various types of tumors. It is known that antifolates are a class of cytotoxic or antineoplastic agents, which inhibit or prevent the maturation and proliferation of malignant cells. Talotrexin was studied in clinical trials for the treatment of brain and central nervous system tumors, leukemia, lymphoma, unspecified childhood solid tumor. However, this study was withdrawn because of toxicity. In addition, was studied in phase I/II multicenter clinical trial in patients with non-small-cell Lung carcinoma, this study was also withdrawn. The withdrawal was related to incidences of dose-limiting mucositis and myelosuppression. However, on May 22, 2006, was announced that the U.S. Food and Drug Administration has granted orphan drug designation for talotrexin in patients with acute lymphoblastic leukemia (ALL).
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Treatment of acute lymphoblastic leukaemia : a new era. | 2007 |
|
Emerging therapeutic options for Philadelphia-positive acute lymphocytic leukemia. | 2007 Mar |
|
Clinical potency of methotrexate, aminopterin, talotrexin and pemetrexed in childhood leukemias. | 2010 May |
|
Cancer chemotherapy: targeting folic acid synthesis. | 2010 Nov 19 |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT00098514
10 mg/m2 dose of PT523 administered day 1 of a 28-day cycle as a 5 minute IV infusion (IV bolus)
Route of Administration:
Intravenous
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
FDA ORPHAN DRUG |
221306
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
||
|
NCI_THESAURUS |
C2153
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
||
|
NCI_THESAURUS |
C511
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
A8E516A20K
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
C29341
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
633713
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
130731
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
8622
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
CHEMBL590985
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
DB06178
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
623017
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
300000037016
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
113857-87-7
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
C085590
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY | |||
|
DTXSID20921223
Created by
admin on Fri Dec 15 16:04:08 GMT 2023 , Edited by admin on Fri Dec 15 16:04:08 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
SALT/SOLVATE (PARENT)