Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C27H30ClFN4O3.ClH |
| Molecular Weight | 549.464 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.C[C@H]1CN([C@H](C)CN1CC2=CC=C(F)C=C2)C(=O)C3=C(Cl)C=C4N(C)C=C(C(=O)C(=O)N(C)C)C4=C3
InChI
InChIKey=FOJUFGQLUOOBQP-MCJVGQIASA-N
InChI=1S/C27H30ClFN4O3.ClH/c1-16-13-33(17(2)12-32(16)14-18-6-8-19(29)9-7-18)26(35)21-10-20-22(25(34)27(36)30(3)4)15-31(5)24(20)11-23(21)28;/h6-11,15-17H,12-14H2,1-5H3;1H/t16-,17+;/m0./s1
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C27H30ClFN4O3 |
| Molecular Weight | 513.004 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Talmapimod is a p38 MAPK kinase inhibitor that inhibits p38 alpha with IC50 value of 9 nM which is 10-times lower then IC50 for p38 beta. Talmapimod was under clinical development for the treatment of Myelodysplastic Syndromes, Multiple Myeloma and Rheumatoid Arthritis (phase II), however, it seems to be discontinued as no longer presents in Janssen's pipeline.
Originator
Approval Year
Doses
| Dose | Population | Adverse events |
|---|---|---|
360 mg multiple, oral Highest studied dose |
unhealthy, ADULT n = 17 Health Status: unhealthy Condition: myelodysplastic syndrome Age Group: ADULT Sex: M+F Population Size: 17 Sources: |
Disc. AE: ALT increased, Atrial fibrillation... AEs leading to discontinuation/dose reduction: ALT increased (5.9%) Sources: Atrial fibrillation (5.9%) ALT increased (grade 3, 5.9%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| ALT increased | 5.9% Disc. AE |
360 mg multiple, oral Highest studied dose |
unhealthy, ADULT n = 17 Health Status: unhealthy Condition: myelodysplastic syndrome Age Group: ADULT Sex: M+F Population Size: 17 Sources: |
| Atrial fibrillation | 5.9% Disc. AE |
360 mg multiple, oral Highest studied dose |
unhealthy, ADULT n = 17 Health Status: unhealthy Condition: myelodysplastic syndrome Age Group: ADULT Sex: M+F Population Size: 17 Sources: |
| ALT increased | grade 3, 5.9% Disc. AE |
360 mg multiple, oral Highest studied dose |
unhealthy, ADULT n = 17 Health Status: unhealthy Condition: myelodysplastic syndrome Age Group: ADULT Sex: M+F Population Size: 17 Sources: |
Sample Use Guides
Myelodysplastic Syndromes: tablets should be administered orally at a dose of 30, 60, 90 or 120 mg thrice daily for 16 weeks. Multiple Myeloma: two 30-mg capsules three times daily. Rheumatoid Arthritis: 30 mg, 60 mg, 90 mg administered dailly for 30 days or 60 mg for one week followed by 120 for one week followed by 180 mg for two weeks.
Route of Administration:
Oral
Bone marrow mononuclear cells (BMMNC) (1 × 10(6)) were cultured in the absence or presence of increasing concentrations of talmapimod (0, 10, 20, 50, 100, 500 nM) for 24h without or with 10 ng/mL LPS. The drug was shown to potently inhibit the secretion of TNFalpha from both basal or LPS-induced cell cultures with an IC50 of 50 nM.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:45:54 GMT 2023
by
admin
on
Fri Dec 15 15:45:54 GMT 2023
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| Record UNII |
K6T0L6I32X
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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309915-12-6
Created by
admin on Fri Dec 15 15:45:54 GMT 2023 , Edited by admin on Fri Dec 15 15:45:54 GMT 2023
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NON-SPECIFIC STOICHIOMETRY | |||
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16035045
Created by
admin on Fri Dec 15 15:45:54 GMT 2023 , Edited by admin on Fri Dec 15 15:45:54 GMT 2023
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PRIMARY | |||
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K6T0L6I32X
Created by
admin on Fri Dec 15 15:45:54 GMT 2023 , Edited by admin on Fri Dec 15 15:45:54 GMT 2023
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PRIMARY |
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |