DEXAMETHASONE ACETATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C24H31FO6.H2O
Molecular Weight	452.513
Optical Activity	UNSPECIFIED
Defined Stereocenters	8 / 8
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O.C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COC(C)=O

InChI

InChIKey=DPHFJXVKASDMBW-RQRKFSSASA-N

InChI=1S/C24H31FO6.H2O/c1-13-9-18-17-6-5-15-10-16(27)7-8-21(15,3)23(17,25)19(28)11-22(18,4)24(13,30)20(29)12-31-14(2)26;/h7-8,10,13,17-19,28,30H,5-6,9,11-12H2,1-4H3;1H2/t13-,17+,18+,19+,21+,22+,23+,24+;/m1./s1

HIDE SMILES / InChI

Description
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004071/WC500204050.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdf
Curator's Comment: description was created based on several sources, including: https://www.drugs.com/pro/dexamethasone.html | http://www.wikidoc.org/index.php/Dexamethasone_(oral) | http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/040572s002lbl.pdf

Dexamethasone is an anti-inflammatory agent that is FDA approved for the treatment of many conditions, including rheumatic problems, a number of skin diseases, severe allergies, asthma, chronic obstructive lung disease, croup, brain swelling and others. Dexamethasone is a glucocorticoid agonist. Unbound dexamethasone crosses cell membranes and binds with high affinity to specific cytoplasmic glucocorticoid receptors. Adverse reactions are: Glaucoma with optic nerve damage, visual acuity and field defects; cataract formation; secondary ocular infection following suppression of host response; and perforation of the globe may occur; muscle weakness; osteoporosis and others. Aminoglutethimide may diminish adrenal suppression by corticosteroids. Macrolide antibiotics have been reported to cause a significant decrease in corticosteroid clearance.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Glucocorticoid receptor 173 Target ID: CHEMBL2034 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10551779 \| https://www.ncbi.nlm.nih.gov/pubmed/16971495 \| https://www.ncbi.nlm.nih.gov/pubmed/2226278	Agonist 2752	4.6 nM [Kd]
Glucocorticoid receptor 173 Target ID: CHEMBL2034 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004071/WC500204050.pdf	Agonist 2752	3.7 nM [Kd]
Mineralocorticoid receptor 53 Target ID: CHEMBL1994 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004071/WC500204050.pdf	Agonist 2752	0.73 nM [Kd]

Conditions

Condition	Modality	Highest Phase	Product
Allergic conjunctivitis 101 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdf	Primary	Approved 8583	MAXIDEX Approved Use For steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date 1962
Acne rosacea 44 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdf	Primary	Approved 8583	MAXIDEX Approved Use Steroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe such as allergic conjunctivitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, selected infective conjunctivitides when the inherent hazard of steroid use is accepted to obtain an advisable diminution in edema and inflammation; corneal injury from chemical, radiation, or thermal burns, or penetration of foreign bodies. Launch Date 1962
Superficial punctate keratitis 43 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdf	Primary	Approved 8583	MAXIDEX Approved Use For steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date 1962
Herpes zoster keratitis 44 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdf	Primary	Approved 8583	MAXIDEX Approved Use For steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date 1962
Iritis 43 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdf	Primary	Approved 8583	MAXIDEX Approved Use For steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date 1962
Cyclitis 21 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdf	Primary	Approved 8583	MAXIDEX Approved Use For steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date 1962
Corneal injury 21 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdf	Primary	Approved 8583	MAXIDEX Approved Use For steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date 1962
Bacterial conjunctivitis 34 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdf	Primary	Approved 8583	MAXIDEX Approved Use For steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date 1962
Multiple myeloma 159 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004071/WC500204050.pdf	Primary	Approved 8583	Neofordex Approved Use Neofordex is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Launch Date 2016

C_max

Value	Dose	Co-administered	Analyte	Population
9.87 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22047811	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:		DEXAMETHASONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
51.2 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22047811	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:		DEXAMETHASONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
3.93 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22047811	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:		DEXAMETHASONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
32% REVIEW https://pubmed.ncbi.nlm.nih.gov/30115648/	unknown, intravenous		DEXAMETHASONE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
30% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3806166			DEXAMETHASONE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
96 mg multiple, oral Dose: 96 mg Route: oral Route: multiple Dose: 96 mg Sources: https://pubmed.ncbi.nlm.nih.gov/31139529	unhealthy, 63 years (range: 30–78 years) Health Status: unhealthy Age Group: 63 years (range: 30–78 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/31139529	Sources: https://pubmed.ncbi.nlm.nih.gov/31139529
0.1 % 3 times / day multiple, ophthalmic Dose: 0.1 %, 3 times / day Route: ophthalmic Route: multiple Dose: 0.1 %, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/25135542	unhealthy, 68.3 years (range: 51.0 - 83.0 years) Health Status: unhealthy Age Group: 68.3 years (range: 51.0 - 83.0 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/25135542	Other AEs: Corneal erosion... Other AEs: Corneal erosion (10%) Sources: https://pubmed.ncbi.nlm.nih.gov/25135542
0.6 mg/kg single, oral Dose: 0.6 mg/kg Route: oral Route: single Dose: 0.6 mg/kg Sources: https://clinicaltrials.gov/ct2/show/NCT02794441	unhealthy, children Health Status: unhealthy Age Group: children Sources: https://clinicaltrials.gov/ct2/show/NCT02794441	Other AEs: Constipation... Other AEs: Constipation (below serious, 1 patient) Sources: https://clinicaltrials.gov/ct2/show/NCT02794441
10 mg single, intravenous Dose: 10 mg Route: intravenous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00122278	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT00122278	Other AEs: Drowsiness, Dizziness... Other AEs: Drowsiness (below serious, 19 patients) Dizziness (below serious, 3 patients) Adverse drug reaction NOS (below serious, 10 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT00122278
12 mg 1 times / day multiple, intravenous Dose: 12 mg, 1 times / day Route: intravenous Route: multiple Dose: 12 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT02271698	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT02271698	Other AEs: Wound dehiscence... Other AEs: Wound dehiscence (below serious, 1 patient) Sources: https://clinicaltrials.gov/ct2/show/NCT02271698
20 mg single, intravenous Dose: 20 mg Route: intravenous Route: single Dose: 20 mg Sources: https://pubmed.ncbi.nlm.nih.gov/33743063	unhealthy Health Status: unhealthy Sources: https://pubmed.ncbi.nlm.nih.gov/33743063	Sources: https://pubmed.ncbi.nlm.nih.gov/33743063
24 mg 1 times / day multiple, intravenous Dose: 24 mg, 1 times / day Route: intravenous Route: multiple Dose: 24 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT02271698	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT02271698	Other AEs: Dizziness... Other AEs: Dizziness (below serious, 1 patient) Sources: https://clinicaltrials.gov/ct2/show/NCT02271698
8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01248585	unhealthy Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT01248585	Other AEs: Constipation, Dyspepsia... Other AEs: Constipation (below serious, 47 patients) Dyspepsia (below serious, 12 patients) Vomiting (below serious, 9 patients) Fatigue (below serious, 58 patients) Cholesterol high (below serious, 8 patients) Anorexia (below serious, 15 patients) Anxiety (below serious, 11 patient) Insomnia (below serious, 26 patients) Cough (below serious, 9 patients) Dyspnea (below serious, 20 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT01248585
8 mg single, intravenous Dose: 8 mg Route: intravenous Route: single Dose: 8 mg Sources: https://clinicaltrials.gov/ct2/show/NCT01734161	pregnant Health Status: pregnant Sex: F Sources: https://clinicaltrials.gov/ct2/show/NCT01734161	Other AEs: Incision site bleeding, Body temperature decrease... Other AEs: Incision site bleeding (below serious, 1 patient) Body temperature decrease (below serious, 2 patients) Shivering (below serious, 1 patient) Tachycardia (below serious, 1 patient) Transfusion (below serious, 1 patient) Sources: https://clinicaltrials.gov/ct2/show/NCT01734161

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087 inhibitor 2252 substrate 1946	inhibitor 2438		inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OATP1B1 1079 BCRP 910 OATP1B3 961 CYP19A1 429 CYP1A2 2153 CYP3A5 136 P-gp 1741 OAT1 725	P-gp 2052	UGT1A1 78 UGT1A5 21 UGT1A6 34 UGT2B1 21 BCRP 101 P-gp 301 OAT1 28 MRP4 53 MRP1 74 MRP2 146 MRP3 83 MRP5 45 ABCC12 43

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP2C9 2497	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/236702#section=Biological-Test-Results Page: 16.0	inconclusive [IC50 15.4871 uM]
ABCC12 43	inducer 1966 Sources: https://www.sciencedirect.com/science/article/pii/S0143400412002895 Page: -	no
BCRP 985	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/236702#section=Biological-Test-Results Page: 62.0	no
CYP19A1 430	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/236702#section=Biological-Test-Results Page: 6.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/236702#section=Biological-Test-Results Page: 302.0	no
CYP3A4 2633	inducer 1966 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/236702#section=Biological-Test-Results Page: 265.0	no
MRP1 232	inducer 1966 Sources: https://www.sciencedirect.com/science/article/pii/S0143400412002895 Page: -	no
MRP2 625	inducer 1966 Sources: https://www.sciencedirect.com/science/article/pii/S0143400412002895 Page: -	no
MRP3 326	inducer 1966 Sources: https://www.sciencedirect.com/science/article/pii/S0143400412002895 Page: -	no
MRP5 80	inducer 1966 Sources: https://www.sciencedirect.com/science/article/pii/S0143400412002895 Page: -	no
OAT1 730	inducer 1966 Sources: https://www.sciencedirect.com/science/article/pii/S1931524413002557 Page: -	no
OAT1 730	inhibitor 4027 Sources: https://www.sciencedirect.com/science/article/pii/S1931524413002557 Page: -	no
UGT1A6 171	inducer 1966 Sources: https://link.springer.com/article/10.1023%2FA%3A1018812021549 Page: -	no
CYP3A5 201	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/34648292/	weak [IC50 >300 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/236702#section=Biological-Test-Results Page: 15.0	yes [IC50 8.709 uM]
OATP1B1 1095	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNjk3NjY4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDE1MzA0MjgifX0=	yes [Inhibition 10 uM]
OATP1B3 970	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNzQzMTIxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDE1MzA0MjgifX0=	yes [Inhibition 10 uM]
BCRP 985	inducer 1966 Sources: https://journals.physiology.org/doi/full/10.1152/ajpcell.00491.2007 Page: -	yes
MRP1 232	activator 342 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/236702#section=Biological-Test-Results Page: 47.0	yes
MRP4 345	inducer 1966 Sources: https://www.sciencedirect.com/science/article/pii/S1931524413002557 Page: -	yes
P-gp 1932	inducer 1966 Sources: https://journals.physiology.org/doi/full/10.1152/ajpcell.00491.2007 Page: -	yes
P-gp 1932	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/236702#section=Biological-Test-Results Page: 21.0	yes
UGT1A1 303	inducer 1966 Sources: https://link.springer.com/article/10.1023/B:MOLE.0000043582.35335.ff Page: -	yes
UGT1A5 21	inducer 1966 Sources: https://link.springer.com/article/10.1023%2FA%3A1018812021549 Page: -	yes
UGT2B1 22	inducer 1966 Sources: https://link.springer.com/article/10.1023%2FA%3A1018812021549 Page: -	yes
CYP3A4 2633	inducer 1966 Sources: https://ascpt.onlinelibrary.wiley.com/doi/full/10.1067/mcp.2000.110215 Page: -	yes	yes (co-administration study) Comment: These data demonstrate that dexamethasone at doses used clinically increased CYP3A4 activity with extensive intersubject variability and that the extent of CYP3A4 induction was, in part, predicted by the baseline activity of CYP3A4 in both healthy volunteers and human hepatocyte cultures. Sources: https://ascpt.onlinelibrary.wiley.com/doi/full/10.1067/mcp.2000.110215 Page: -

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/236702#section=Biological-Test-Results Page: 258 \| 259	no
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/17124593/ Page: -	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/236702#section=Biological-Test-Results Page: 301.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:41879	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:41879
ChemicalBook	CB4261243	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB4261243
eMolecules	29541178	https://www.emolecules.com/cgi-bin/more?vid=29541178
eMolecules	30067429	https://www.emolecules.com/cgi-bin/more?vid=30067429
eMolecules	31411022	https://www.emolecules.com/cgi-bin/more?vid=31411022
eMolecules	497104	https://www.emolecules.com/cgi-bin/more?vid=497104
MolPort	MolPort-003-846-433	https://www.molport.com/shop/molecule-link/MolPort-003-846-433
Selleck Chemicals	Dexamethasone	http://www.selleckchem.com/products/Dexamethasone.html
ZINC	ZINC000003875332	http://zinc15.docking.org/substances/ZINC000003875332

PubMed

Title	Date	PubMed
CEP-18770 (delanzomib) in combination with dexamethasone and lenalidomide inhibits the growth of multiple myeloma.	2012-11	22906694
Triptolide enhances the sensitivity of multiple myeloma cells to dexamethasone via microRNAs.	2012-06	22260163
Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity with dexamethasone.	2012-06	22207485
Genomic screening for genes silenced by DNA methylation revealed an association between RASD1 inactivation and dexamethasone resistance in multiple myeloma.	2009-07-01	19549772
Combining milatuzumab with bortezomib, doxorubicin, or dexamethasone improves responses in multiple myeloma cell lines.	2009-04-15	19351768
A multicenter, randomized open study of early corticosteroid treatment (OSECT) in preterm infants with respiratory illness: comparison of early and late treatment and of dexamethasone and inhaled budesonide.	2001-02	11158452
Adverse effects of early dexamethasone treatment in extremely-low-birth-weight infants. National Institute of Child Health and Human Development Neonatal Research Network.	2001-01-11	11150359
Intractable nausea attributable to isolated deficiency of adrenocorticotropic hormone: prompt resolution after administration of glucocorticoid.	2001-01-06	11141589
Molecular and pharmacological evidence for modulation of kinin B(1) receptor expression by endogenous glucocorticoids hormones in rats.	2001-01	11159707
Evaluation of the myocilin (MYOC) glaucoma gene in monkey and human steroid-induced ocular hypertension.	2001-01	11133859
The clinical impact of metabolic bone disease in coeliac disease.	2001-01	11123392
Short term effects of corticosteroid pulse treatment on disease activity and the wellbeing of patients with active rheumatoid arthritis.	2001-01	11114284
Inhibition of NF-kappaB and AP-1 activation by R- and S-flurbiprofen.	2001-01	11099482
Topical 0.1% indomethacin solution versus topical 0.1% dexamethasone solution in the prevention of inflammation after cataract surgery. The Study Group.	2000-12-23	11125269
Prenatal exposure to high levels of glucocorticoids increases the susceptibility of cerebellar granule cells to oxidative stress-induced cell death.	2000-12-19	11114198
Low doses of oral dexamethasone for hormone-refractory prostate carcinoma.	2000-12-15	11135218
Suppressive effect of active hexose correlated compound (AHCC) on thymic apoptosis induced by dexamethasone in the rat.	2000-12	11137978
Effect of endogenous and exogenous prostaglandin E(2) on interleukin-1 beta-induced cyclooxygenase-2 expression in human airway smooth-muscle cells.	2000-12	11112151
Ritonavir increases the level of active ADD-1/SREBP-1 protein during adipogenesis.	2000-11-10	11101056
Regulation of leptin release by troglitazone in human adipose tissue.	2000-11	11092516
Ocular hypertensive response to topical dexamethasone in children: a dose-dependent phenomenon.	2000-11	11054340
Efficacy of galectins in the amelioration of nephrotoxic serum nephritis in Wistar Kyoto rats.	2000-11	11044214
Dexamethasone-induced cardiogenic shock rescued by percutaneous cardiopulmonary support (PCPS) in a patient with pheochromocytoma.	2000-10	11059621
Antenatal dexamethasone enhances surfactant protein synthesis in the hypoplastic lung of nitrofen-induced diaphragmatic hernia in rats.	2000-10	11051153
Role of caspases in dexamethasone-induced apoptosis and activation of c-Jun NH2-terminal kinase and p38 mitogen-activated protein kinase in human eosinophils.	2000-10	11012613
Endotoxin augments cerebral hyperemic response to halothane by inducing nitric oxide synthase and cyclooxygenase.	2000-10	11004044
Involvement of tyrosine hydroxylase up regulation in dexamethasone-induced hypertension of rats.	2000-09-08	11072875
Endocrinologic and psychological effects of short-term dexamethasone in anorexia nervosa.	2000-09	11082797
ECT administration in a patient after craniotomy and gamma knife surgery: a case report and review.	2000-09	11005053
Modification of biophysical properties of lung epithelial Na(+) channels by dexamethasone.	2000-09	10942727
Dexamethasone-suppressible hypertension.	2000-08-26	11085685
Effects of dexamethasone on mitogen-activated protein kinases in mouse macrophages: implications for the regulation of 85 kDa cytosolic phospholipase A(2).	2000-08-15	10874129
TEL/AML1 gene fusion is related to in vitro drug sensitivity for L-asparaginase in childhood acute lymphoblastic leukemia.	2000-08-01	10910927
Leptin production in adipocytes from morbidly obese subjects: stimulation by dexamethasone, inhibition with troglitazone, and influence of gender.	2000-08	10946865
Dexamethasone enhances ras-recision gene expression in cultured murine fetal lungs: role in development.	2000-08	10926554
Dexamethasone suppresses tumor necrosis factor-alpha-induced apoptosis in osteoblasts: possible role for ceramide.	2000-08	10919278
Effects of several glucocorticosteroids and PDE4 inhibitors on increases in total lung eosinophil peroxidase (EPO) levels following either systemic or intratracheal administration in sephadex- or ovalbumin-induced inflammatory models.	2000-08	10850854
Efficacy and harm of pharmacological prevention of acute mountain sickness: quantitative systematic review.	2000-07-29	10915127
Cognitive sequelae in children treated for acute lymphoblastic leukemia with dexamethasone or prednisone.	2000-06-23	10864051
Corticosteroids and cognitive function in humans: methodological considerations.	2000-06-23	10864049
Dexamethasone induced cardiac hypertrophy in newborn rats is accompanied by changes in myosin heavy chain phenotype and gene transcription.	2000-06	10942214
Expression and induction of CYP1A1/1A2, CYP2A6 and CYP3A4 in primary cultures of human hepatocytes: a 10-year follow-up.	2000-06	10923861
Combined administration of G-CSF and dexamethasone for the mobilization of granulocytes in normal donors: optimization of dosing.	2000-06	10864982
Down-regulation of thyroid transcription factor-1 gene expression in fetal lung hypoplasia is restored by glucocorticoids.	2000-06	10830305
Effects of selected herbicides on cytokine production in vitro.	2000-05-19	10883730
Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands.	2000-05-19	10748001
Glucocorticoids act within minutes to inhibit recruitment of signalling factors to activated EGF receptors through a receptor-dependent, transcription-independent mechanism.	2000-05	10807665
Effect of polyunsaturated fatty acids on dexamethasone-induced gastric mucosal damage.	2000-02	10780873
Antenatal dexamethasone improves atrial natriuretic peptide receptors in hypoplastic lung in nitrofen-induced diaphragmatic hernia in rats.	2000	10898224
Blockade of cocaine-induced increases in adrenocorticotrophic hormone and cortisol does not attenuate the subjective effects of smoked cocaine in humans.	1999-09	10780258

Patents

Sample Use Guides

In Vivo Use Guide

The dose and administration frequency varies with the therapeutic protocol and the associated treatment(s). The usual posology of NEOFORDEX® is 40 mg once per day of administration.

Route of Administration: Oral

In Vitro Use Guide

The effects on apoptosis and related signaling pathways in the t(4;14)+ multiple myeloma (MM) subset, applying drug combinations including a FGFR3 tyrosine kinase inhibitor (RTKI), the proteasome inhibitor bortezomib, and dexamethasone were tested. RTKI, bortezomib, and dexamethasone were active as single agents in t(4;14)+ MM. RTK inhibition triggered complementary proapoptotic pathways (e.g., decrease of antiapoptotic Mcl-1 protein, down-regulation of p44/42 mitogen-activated protein kinase, and activation of proapoptotic stress-activated protein/c-Jun NH(2)-terminal kinases). Synergistic or additive effects were found by combinations of RTKI with dexamethasone or bortezomib. In t(4;14)+, N-ras-mutated NCI-H929 cells, resistance to RTKI was overcome by addition of dexamethasone. Notably, the combination of RTKI and dexamethasone showed additive proapoptotic effects in bortezomib-insensitive t(4;14)+ MM.

Name

Type

Language

DEXAMETHASONE ACETATE MONOHYDRATE

Preferred Name

English

DEXAMETHASONE ACETATE

Official Name

English

PREGNA-1,4-DIENE-3,20-DIONE, 21-(ACETYLOXY)-9-FLUORO-11,17-DIHYDROXY-16-METHYL-, (11.BETA.,16.ALPHA.)-, MONOHYDRATE

Systematic Name

English

9-Fluoro-11?,17,21-trihydroxy-16?-methylpregna-1,4-diene-3,20-dione 21-acetate, monohydrate

Systematic Name

English

DEXAMETHASONI ACETAS MONOHYDRATE [WHO-IP LATIN]

Common Name

English

DEXAMETHASONE ACETATE, MONOHYDRATE

Common Name

English

DEXAMETHASONE ACETATE [JAN]

Common Name

English

Dexamethasone acetate monohydrate [WHO-DD]

Common Name

English

DEXAMETHASONE ACETATE MONOHYDRATE [ORANGE BOOK]

Common Name

English

DEXAMETHASONE ACETATE MONOHYDRATE [WHO-IP]

Common Name

English

DEXAMETHASONE ACETATE [USAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C521