Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C32H38N2O5 |
Molecular Weight | 530.6545 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12C[C@@H](C)[C@](O)(C(=O)COC(C)=O)[C@@]1(C)C[C@H](O)[C@@]3([H])[C@@]2([H])C=C(C)C4=CC5=C(C[C@]34C)C=NN5C6=CC=CC=C6
InChI
InChIKey=RKHQGWMMUURILY-UHRZLXHJSA-N
InChI=1S/C32H38N2O5/c1-18-11-23-25-12-19(2)32(38,28(37)17-39-20(3)35)31(25,5)15-27(36)29(23)30(4)14-21-16-33-34(26(21)13-24(18)30)22-9-7-6-8-10-22/h6-11,13,16,19,23,25,27,29,36,38H,12,14-15,17H2,1-5H3/t19-,23+,25+,27+,29-,30+,31+,32+/m1/s1
Molecular Formula | C32H38N2O5 |
Molecular Weight | 530.6545 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 7 / 8 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
The phenylpyrazosteroid cortivazol is a selective agonist ligand for the glucocorticoid receptor (GR), a steroid receptor member of the nuclear receptor superfamily of transcription factors. Cortivazol is an apoptotic, anti-inflammatory and immunosuppressive agent that has been used in the treatment of diskogenic radiculopathy, back pain, osteoarthritis and acute childhood lymphoblastic leukemia. Cortivazol has potent antileukemic activity in childhood ALL. Its activity is related to cell cycle arrest and induction of apoptosis. Cortivazol (Altim) is indicated in rheumatological diseases:
- In intra-articular injection: inflammatory arthritis, advanced osteoarthritis.
- In periarticular injection: tendinitis, bursitis.
- In injection of soft tissue: talalgia, carpal tunnel syndrome, Dupuytren’s contracture.
- In epidural injection: radiculalgia
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | ALTIM Approved UseThis product is indicated in rheumatological diseases:
- In intra-articular injection: inflammatory arthritis, advanced osteoarthritis.
- In periarticular injection: tendinitis, bursitis.
- In injection of soft tissue: talalgia, carpal tunnel syndrome, Dupuytren’s contracture.
- In epidural injection: radiculalgia |
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Primary | ALTIM Approved UseThis product is indicated in rheumatological diseases:
- In intra-articular injection: inflammatory arthritis, advanced osteoarthritis.
- In periarticular injection: tendinitis, bursitis.
- In injection of soft tissue: talalgia, carpal tunnel syndrome, Dupuytren’s contracture.
- In epidural injection: radiculalgia |
PubMed
Title | Date | PubMed |
---|---|---|
[Superficial injections of anti-inflammatory drugs and severe infectious complications]. | 2001 May 5-12 |
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Distinct interaction of cortivazol with the ligand binding domain confers glucocorticoid receptor specificity: cortivazol is a specific ligand for the glucocorticoid receptor. | 2002 Feb 15 |
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Better results with rhenium-186 radiosynoviorthesis than with cortivazol in rheumatoid arthritis (RA): a two-year follow-up randomized controlled multicentre study. | 2004 Sep-Oct |
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The distinct agonistic properties of the phenylpyrazolosteroid cortivazol reveal interdomain communication within the glucocorticoid receptor. | 2005 May |
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Intraarticular glucocorticoid injections in rapidly destructive hip osteoarthritis. | 2006 Jan |
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High risk of adrenal insufficiency after a single articular steroid injection in athletes. | 2007 Jul |
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Injection therapy and denervation procedures for chronic low-back pain: a systematic review. | 2010 Sep |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://en.pharmacodia.com/web/drug/1_11814.html
300 ugrams of cortivazol is equivalent in anti-inflammatory activity to about 5 mg of prednisolone. It is given in the treatment of musculoskeletal and joint disorders by intra-articular, periarticular, or epidural injection in doses of about 1.25 to 3.75 mg, usually at intervals of 1 to 3 weeks.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2880860
Incubation of ICR 27 cells with cortivazol caused 50% growth inhibition and 50% maximal induction of glutamine synthetase activity at concentrations of 20 and 35 nM, respectively.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:16:27 UTC 2023
by
admin
on
Fri Dec 15 15:16:27 UTC 2023
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Record UNII |
YM183K0H63
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Record Status |
Validated (UNII)
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NCI_THESAURUS |
C521
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QH02AB17
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H02AB17
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1110-40-3
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80998
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100000084250
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Cortivazol
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214-175-8
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YM183K0H63
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C005924
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C80812
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66249
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m3797
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DB13003
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DTXSID40149442
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