Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H25NO4 |
| Molecular Weight | 343.4168 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(OC2CCCC2)C=C(C=C1)[C@]3(CC[C@@H](CC3)C(O)=O)C#N
InChI
InChIKey=CFBUZOUXXHZCFB-OYOVHJISSA-N
InChI=1S/C20H25NO4/c1-24-17-7-6-15(12-18(17)25-16-4-2-3-5-16)20(13-21)10-8-14(9-11-20)19(22)23/h6-7,12,14,16H,2-5,8-11H2,1H3,(H,22,23)/t14-,20-
| Molecular Formula | C20H25NO4 |
| Molecular Weight | 343.4168 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: Description is created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/11772257 and http://www.drugdevelopment-technology.com/projects/ariflo/
Curator's Comment: Description is created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/11772257 and http://www.drugdevelopment-technology.com/projects/ariflo/
Cilomilast (Ariflo) is an oral selective phosphodiesterase (PDE) IV inhibitor under development by GlaxoSmithKline Pharmaceuticals for treatment of COPD. After the demise of Merck's PDE-IV inhibitor (licensed from Celltech Group) in April 2003, Ariflo has emerged as the frontrunner in this new class of agents for inflammatory airways diseases, such as COPD. GlaxoSmithKline filed for drug approval with the US FDA at the end of 2002 and in January 2003 with the European Medicines Evaluation Agency (EMEA). In October 2003 the FDA issued an approvable letter for use of Ariflo in maintenance of lung function in COPD patients poorly responsive to salbutamol, despite an earlier decision by the FDA advisory panel to reject approval. Cilomilast shows high selectivity for cAMP-specific PDE4, an isoenzyme that predominates in pro-inflammatory and immune cells and that is 10-fold more selective for PDE4D than for PDE4A, -B or -C. In vitro, cilomilastsuppresses the activity of several pro-inflammatory and immune cells that have been implicated in the pathogenesis of asthma and COPD. Moreover, it is highly active in animal models of these diseases. Cilomilast has been shown to exert potent anti-inflammatory effects both in vitro and in vivo.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: GO:0042554 Sources: http://www.ncbi.nlm.nih.gov/pubmed/22041526 |
96.0 nM [IC50] | ||
Target ID: CHEMBL288 Sources: http://www.ncbi.nlm.nih.gov/pubmed/17155857 |
12.0 nM [IC50] | ||
Target ID: CHEMBL254 Sources: http://www.ncbi.nlm.nih.gov/pubmed/17155857 |
115.0 nM [IC50] | ||
Target ID: CHEMBL275 Sources: http://www.ncbi.nlm.nih.gov/pubmed/17155857 |
86.0 nM [IC50] | ||
Target ID: CHEMBL291 Sources: http://www.ncbi.nlm.nih.gov/pubmed/17155857 |
308.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | ARIFLO Approved UseARIFLO is intended to be used regularly as maintenance therapy for the the treatment of chronic obstructive pulmonary disease (COPD). Launch Date2003 |
|||
Sources: http://www.ncbi.nlm.nih.gov/pubmed/11772257 |
Primary | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.248 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.463 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.872 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.122 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.186 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1.68 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.281 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
2 mg 2 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.596 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
4 mg 2 times / day steady-state, oral dose: 4 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1.09 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
7 mg 2 times / day steady-state, oral dose: 7 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1.48 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
10 mg 2 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.66 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
15 mg 2 times / day steady-state, oral dose: 15 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.08 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.91 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
5.04 pmol × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.78 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
12.2 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
13.4 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1.43 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
2 mg 2 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
3.06 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
4 mg 2 times / day steady-state, oral dose: 4 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.01 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
7 mg 2 times / day steady-state, oral dose: 7 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.94 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
10 mg 2 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
13.9 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
15 mg 2 times / day steady-state, oral dose: 15 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3.27 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.76 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.69 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
7.19 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
7.04 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.16 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
2 mg 2 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
8.11 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
4 mg 2 times / day steady-state, oral dose: 4 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
8.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
7 mg 2 times / day steady-state, oral dose: 7 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
7.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
10 mg 2 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
8.24 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16509757/ |
15 mg 2 times / day steady-state, oral dose: 15 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.5% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11549099/ |
CILOMILAST plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
30 mg 2 times / day steady-state, oral Highest studied dose Dose: 30 mg, 2 times / day Route: oral Route: steady-state Dose: 30 mg, 2 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FED Sources: |
|
15 mg 2 times / day multiple, oral Studied dose Dose: 15 mg, 2 times / day Route: oral Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
Disc. AE: Abdominal pain, Dyspepsia... AEs leading to discontinuation/dose reduction: Abdominal pain Sources: Dyspepsia Nausea |
15 mg 2 times / day multiple, oral Studied dose Dose: 15 mg, 2 times / day Route: oral Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
Disc. AE: Atrial flutter, Gastritis... AEs leading to discontinuation/dose reduction: Atrial flutter Sources: Gastritis Gastroesophageal reflux disease Nausea Enteritis |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Abdominal pain | Disc. AE | 15 mg 2 times / day multiple, oral Studied dose Dose: 15 mg, 2 times / day Route: oral Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Dyspepsia | Disc. AE | 15 mg 2 times / day multiple, oral Studied dose Dose: 15 mg, 2 times / day Route: oral Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Nausea | Disc. AE | 15 mg 2 times / day multiple, oral Studied dose Dose: 15 mg, 2 times / day Route: oral Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Atrial flutter | Disc. AE | 15 mg 2 times / day multiple, oral Studied dose Dose: 15 mg, 2 times / day Route: oral Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Enteritis | Disc. AE | 15 mg 2 times / day multiple, oral Studied dose Dose: 15 mg, 2 times / day Route: oral Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Gastritis | Disc. AE | 15 mg 2 times / day multiple, oral Studied dose Dose: 15 mg, 2 times / day Route: oral Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Gastroesophageal reflux disease | Disc. AE | 15 mg 2 times / day multiple, oral Studied dose Dose: 15 mg, 2 times / day Route: oral Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Nausea | Disc. AE | 15 mg 2 times / day multiple, oral Studied dose Dose: 15 mg, 2 times / day Route: oral Route: multiple Dose: 15 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| PDE4B5, a novel, super-short, brain-specific cAMP phosphodiesterase-4 variant whose isoform-specifying N-terminal region is identical to that of cAMP phosphodiesterase-4D6 (PDE4D6). | 2007-08 |
|
| L-454,560, a potent and selective PDE4 inhibitor with in vivo efficacy in animal models of asthma and cognition. | 2007-06-15 |
|
| Therapeutic benefit of PDE4 inhibitors in inflammatory diseases. | 2007-05 |
|
| Effects of cyclosporin A and cilomilast on activated canine, murine and human keratinocytes. | 2007-04 |
|
| Highly selective phosphodiesterase 4 inhibitors for the treatment of allergic skin diseases and psoriasis. | 2007-03 |
|
| Phosphodiesterase-4 inhibitors as a novel approach for the treatment of respiratory disease: cilomilast. | 2007-01 |
|
| Evaluation of oral corticosteroids and phosphodiesterase-4 inhibitor on the acute inflammation induced by inhaled lipopolysaccharide in human. | 2007 |
|
| Selective inhibitors for phosphodiesterase 3 and 4 in antigen-induced increase of cough reflex sensitivity in guinea pigs. | 2007 |
|
| The phosphodiesterase type IV inhibitor cilomilast decreases pro-inflammatory cytokine production from primary bronchial epithelial cells in lung transplantation patients. | 2006-12 |
|
| Phosphodiesterase 4 inhibition of beta2-integrin adhesion caused by leukotriene B4 and TNF-alpha in human neutrophils. | 2006-11 |
|
| Phosphodiesterase 4 inhibitors modulate beta2-adrenoceptor agonist-induced human airway hyperresponsiveness. | 2006-10-12 |
|
| Effects of ciclamilast, a new PDE 4 PDE4 inhibitor, on airway hyperresponsiveness, PDE4D expression and airway inflammation in a murine model of asthma. | 2006-10-10 |
|
| Cilomilast: orally active selective phosphodiesterase-4 inhibitor for treatment of chronic obstructive pulmonary disease. | 2006-10 |
|
| Determination of drug binding to plasma proteins using competitive equilibrium binding to dextran-coated charcoal. | 2006-10 |
|
| Gateways to clinical trials. | 2006-08-09 |
|
| An update and appraisal of the cilomilast Phase III clinical development programme for chronic obstructive pulmonary disease. | 2006-08 |
|
| Involvement of MMP-12 and phosphodiesterase type 4 in cigarette smoke-induced inflammation in mice. | 2006-06 |
|
| Preferential inhibition of human phosphodiesterase 4 by ibudilast. | 2006-05-01 |
|
| Roflumilast for the treatment of chronic obstructive pulmonary disease. | 2006-05 |
|
| [Pharmacological treatment of COPD and future of anti-inflammatory therapy]. | 2006-04-15 |
|
| Effects of cilomilast, a selective phosphodiesterase 4 inhibitor, on esophageal motility and pH, and orocecal and colonic transit: two single-center, randomized, double-blind, placebo-controlled, two-part crossover studies in healthy volunteers. | 2006-04 |
|
| Cilomilast. | 2006-04 |
|
| Phosphodiesterase inhibitors in airways disease. | 2006-03-08 |
|
| Phosphodiesterase type 4 expression and anti-proliferative effects in human pulmonary artery smooth muscle cells. | 2006-01-19 |
|
| Cilomilast for COPD: results of a 6-month, placebo-controlled study of a potent, selective inhibitor of phosphodiesterase 4. | 2006-01 |
|
| COPD, inflammation and its modulation by phosphodiesterase 4 inhibitors: time to look beyond the FEV1. | 2006-01 |
|
| Phosphodiesterase 4 inhibitors for the treatment of asthma and COPD. | 2006 |
|
| The potential role of phosphodiesterase inhibitors in the management of asthma. | 2006 |
|
| Clinical pharmacology of Cilomilast. | 2006 |
|
| Inhibition of airway hyperresponsiveness and pulmonary inflammation by roflumilast and other PDE4 inhibitors. | 2006 |
|
| Cilomilast, tacrolimus and rapamycin modulate dendritic cell function in the elicitation phase of allergic contact dermatitis. | 2005-07 |
|
| Research on airway inflammation: present status in Mainland China. | 2005-06-20 |
|
| Evidence for a role of phosphodiesterase 4 in lipopolysaccharide-stimulated prostaglandin E2 production and matrix metalloproteinase-9 activity in human amniochorionic membranes. | 2005-06-15 |
|
| PDE4 inhibitors as new anti-inflammatory drugs: effects on cell trafficking and cell adhesion molecules expression. | 2005-06 |
|
| Identification and characterization of PDE4A11, a novel, widely expressed long isoform encoded by the human PDE4A cAMP phosphodiesterase gene. | 2005-06 |
|
| Cilomilast GlaxoSmithKline. | 2005-05 |
|
| CGH2466, a combined adenosine receptor antagonist, p38 mitogen-activated protein kinase and phosphodiesterase type 4 inhibitor with potent in vitro and in vivo anti-inflammatory activities. | 2005-04 |
|
| Selective PDE4 inhibitors as potent anti-inflammatory drugs for the treatment of airway diseases. | 2005-03 |
|
| Selective phosphodiesterase-4 inhibitors in chronic obstructive lung disease. | 2005-03 |
|
| Phosphodiesterase 4 inhibition decreases MUC5AC expression induced by epidermal growth factor in human airway epithelial cells. | 2005-02 |
|
| Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease. | 2005-01-11 |
|
| Phosphodiesterase-4: selective and dual-specificity inhibitors for the therapy of chronic obstructive pulmonary disease. | 2005 |
|
| Potentiation and prolongation of long-term odor memory in neonate rats using a phosphodiesterase inhibitor. | 2005 |
|
| The effect of selective phosphodiesterase isoenzyme inhibition on neutrophil function in vitro. | 2005 |
|
| The novel phosphodiesterase 4 inhibitor, CI-1044, inhibits LPS-induced TNF-alpha production in whole blood from COPD patients. | 2005 |
|
| Phosphodiesterase 4-selective inhibition: novel therapy for the inflammation of COPD. | 2005 |
|
| Structural basis for the activity of drugs that inhibit phosphodiesterases. | 2004-12 |
|
| Effects of phosphodiesterase 4 inhibitor on cough response in guinea pigs sensitized and challenged with ovalbumin. | 2004-11 |
|
| TARC and RANTES, but not CTACK, are induced in two models of allergic contact dermatitis. Effects of cilomilast and diflorasone diacetate on T-cell-attracting chemokines. | 2004-10 |
|
| Highly potent PDE4 inhibitors with therapeutic potential. | 2004-09-01 |
Sample Use Guides
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/12034568
10 uM Cilomilast inhibited the chemotaxis of human fetal lung fibroblasts (HFL-1) toward fibronectin in the blindwell assay system
| Substance Class |
Chemical
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| Record UNII |
8ATB1C1R6X
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Validated (UNII)
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C744
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DB03849
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100000092735
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C433247
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153259-65-5
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8ATB1C1R6X
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CILOMILAST
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C95232
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SUB01296MIG
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admin on Mon Mar 31 18:05:39 GMT 2025 , Edited by admin on Mon Mar 31 18:05:39 GMT 2025
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JJ-16
Created by
admin on Mon Mar 31 18:05:39 GMT 2025 , Edited by admin on Mon Mar 31 18:05:39 GMT 2025
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151170
Created by
admin on Mon Mar 31 18:05:39 GMT 2025 , Edited by admin on Mon Mar 31 18:05:39 GMT 2025
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CHEMBL511115
Created by
admin on Mon Mar 31 18:05:39 GMT 2025 , Edited by admin on Mon Mar 31 18:05:39 GMT 2025
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m3549
Created by
admin on Mon Mar 31 18:05:39 GMT 2025 , Edited by admin on Mon Mar 31 18:05:39 GMT 2025
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