clocortolone pivalate: topical, anti-inflammatory glucocorticoid; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
clocortolone pivalate : The 21-O-pivalate ester of clocortolone. It is used for the relief of inflammatory and pruritic (itching) skin disorders. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 5282493 |
| CHEMBL ID | 1200975 |
| CHEBI ID | 59583 |
| SCHEMBL ID | 5120 |
| MeSH ID | M0050050 |
| Synonym |
|---|
| MLS002154165 , |
| smr001233464 |
| BRD-K38003476-001-03-4 |
| BPBIO1_001383 |
| NCGC00179239-01 |
| PRESTWICK3_001119 |
| BSPBIO_001258 |
| PRESTWICK2_001119 |
| AB00514058 |
| cloderm (tn) |
| clocortolone pivalate (usp) |
| 34097-16-0 |
| D02287 |
| pregna-1,4-diene-3,20-dione, 9-chloro-21-(2,2-dimethyl-1-oxopropoxy)-6-fluoro-11-hydroxy-16-methyl-, (6alpha,11beta,16alpha)- |
| clocortolone pivalate [usan] |
| einecs 251-826-5 |
| 9alpha-chloro-6alpha-fluoro-11beta,21-dihydroxy-16alpha-methylpregna-1,4-diene-3,20-dione 21-pivalate |
| sh 863 |
| 9-chloro-6alpha-fluoro-11beta,21-dihydroxy-16alpha-methylpregna-1,4-diene-3,20-dione 21-pivalate |
| clocortolone 21-pivalate |
| clocortolone pivalate |
| cloderm |
| PRESTWICK1_001119 |
| PRESTWICK0_001119 |
| SPBIO_003119 |
| sh-863 |
| CHEMBL1200975 |
| CHEBI:59583 , |
| 9-chloro-6alpha-fluoro-11beta-hydroxy-16alpha-methyl-3,20-dioxopregna-1,4-dien-21-yl 2,2-dimethylpropanoate |
| HMS1571O20 |
| HMS2098O20 |
| [2-[(6s,8s,9r,10s,11s,13s,14s,16r,17s)-9-chloro-6-fluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-7,8,11,12,14,15,16,17-octahydro-6h-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] 2,2-dimethylpropanoate |
| dtxcid8025460 |
| tox21_110632 |
| dtxsid0045460 , |
| HMS2236M06 |
| unii-qbl8izh14x |
| purantix |
| qbl8izh14x , |
| cilder |
| clocortolone pivalate [usan:usp] |
| cl 68 |
| pregna-1,4-diene-3,20-dione, 9-chloro-21-(2,2-dimethyl-1-oxopropoxy)-6-fluoro-11-hydroxy-16-methyl-, (6.alpha.,11.beta.,16.alpha.)- |
| clocortolone pivalate [usp-rs] |
| clocortolone pivalate [orange book] |
| clocortolone pivalate [who-dd] |
| clocortolone 21-pivalate [mi] |
| clocortolone pivalate [usp monograph] |
| clocortolone pivalate [mart.] |
| clocortolone pivalate [vandf] |
| CCG-221119 |
| SCHEMBL5120 |
| clocortolone trimethylacetate |
| SR-01000838872-2 |
| sr-01000838872 |
| clocortolone pivalate (200 mg) |
| HMS3715O20 |
| Q39045318 |
| clocortolone-pivalate |
| NCGC00179239-05 |
| 9-chloro-6|a-fluoro-11|a,21-dihydroxy-16|a-methylpregna-1,4-diene-3,20-dione 21-pivalate pound clocortolone pivalate) |
| CS-0026393 |
| (6alpha,11beta,16alpha)-9-chloro-21-(2,2-dimethyl-1-oxopropoxy)-6-fluoro-11-hydroxy-16-methypregna-1,4-diene-3,20-dione |
| clocortolone pivalate (usan:usp) |
| clocortolone pivalate (usp-rs) |
| clocortolone pivalate cream |
| 9 alpha-chloro-6 alpha-fluoro-11 beta,21-dihydroxy-16 alpha-methylpregna-1,4-diene-3,20-dione 21-pivalate |
| clocortolone pivalate (usp monograph) |
| clocortolone pivalate (mart.) |
| HY-106714 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Role | Description |
|---|---|
| anti-inflammatory drug | A substance that reduces or suppresses inflammation. |
| antipruritic drug | A drug, usually applied topically, that relieves pruritus (itching). |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| glucocorticoid | Glucocorticoids are a class of steroid hormones that regulate a variety of physiological processes, in particular control of the concentration of glucose in blood. |
| 11beta-hydroxy steroid | Any 11-hydroxy steroid in which the hydroxy group at position 11 has beta- configuration. |
| pivalate ester | A carboxylic ester of pivalic acid. |
| 20-oxo steroid | An oxo steroid carrying an oxo group at position 20. |
| fluorinated steroid | A steroid which is substituted with one or more fluorine atoms in any position. |
| 3-oxo-Delta(1),Delta(4)-steroid | A 3-oxo-Delta(1) steroid containing an additional double bond between positions 4 and 5. |
| chlorinated steroid | A steroid which is substituted with one or more chlorine atoms in any position. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 3.1623 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
| AR protein | Homo sapiens (human) | Potency | 0.0686 | 0.0002 | 21.2231 | 8,912.5098 | AID743036; AID743040; AID743042; AID743053; AID743054 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 0.0211 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 0.0473 | 0.0002 | 29.3054 | 16,493.5996 | AID743091 |
| IDH1 | Homo sapiens (human) | Potency | 0.8199 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 0.0596 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 2.8184 | 0.1000 | 9.1916 | 31.6228 | AID1346983 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 0.0065 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| virion membrane | Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 3 (14.29) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (14.29) | 29.6817 |
| 2010's | 13 (61.90) | 24.3611 |
| 2020's | 2 (9.52) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 6 (28.57%) | 5.53% |
| Reviews | 1 (4.76%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 14 (66.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Single Exposure Bioequivalence Study to Evaluate the Vasoconstriction Activity of Topically Applied Cloderm® (Clocortolone Pivalate) 0.1% Cream and Clocortolone Pivalate 0.1% Cream (Taro Pharmaceuticals) in Healthy Male and Female Volunteers With Normal S [NCT04358770] | Phase 1 | 124 participants (Actual) | Interventional | 2018-03-02 | Completed | ||
| An Open-Label, Multicenter Study of the Efficacy of Cloderm® Cream (Clocortolone Pivalate, 0.1%) in the Treatment of Moderate Plaque Psoriasis for 28 Days [NCT01714544] | Phase 4 | 60 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||