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

Molecular Formula	C24H31FO6
Molecular Weight	434.4977
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	8 / 8
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	H2O
Molecular Weight	18.0153
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

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
Effect of antenatal glucocorticoid administration on insulin-like growth factor I and II levels in hypoplastic lung in nitrofen-induced congenital diaphragmatic hernia in rats.	1999	10370016
The role of pulmonary inflammation in the development of pulmonary hypertension in newborn with meconium aspiration syndrome (MAS).	1999	10093144
ECC-1 human endometrial cells as a model system to study dioxin disruption of steroid hormone function.	1999 Apr	10478797
Overexpression of urokinase-type plasminogen activator in pancreatic adenocarcinoma is regulated by constitutively activated RelA.	1999 Aug 12	10467400
Antiemetic efficacy of granisetron plus dexamethasone in bone marrow transplant patients receiving chemotherapy and total body irradiation.	1999 Feb	10084258
Dexamethasone induced alterations in the levels of proteases involved in blood pressure homeostasis and blood coagulation in rats.	1999 Jul	10485340
[Iatrogenic Cushing syndrome and mutatio tarda caused by dexamethasone containing nose drops].	1999 Jul	10463118
Platelet-activating factor receptor mRNA is localized in eosinophils and epithelial cells in rat small intestine: regulation by dexamethasone and gut flora.	1999 Jul	10447766
Structure, evolution, and liver-specific expression of sterol 12alpha-hydroxylase P450 (CYP8B).	1999 Jul	10393316
Effects of inhaled beclomethasone compared to systemic dexamethasone on lung inflammation in preterm infants at risk of chronic lung disease.	1999 Jun	10380089
Differential regulation of peptide alpha-amidation by dexamethasone and disulfiram.	1999 Jun	10347250
The anti-emetic efficacy of tropisetron plus dexamethasone in patients treated with high-dose chemotherapy and stem cell transplantation.	1999 Mar	10089087
Effect of dexamethasone on cyclophosphamide-induced cystitis in rats: lack of relation with bradykinin B1 receptor-mediated motor responses.	1999 Mar 12	10204687
Early (4-7 days of age) dexamethasone therapy for prevention of chronic lung disease in preterm infants.	1999 Nov	10516395
Pharmacological and histopathological study of cyclophosphamide-induced hemorrhagic cystitis - comparison of the effects of dexamethasone and Mesna.	1999 Oct	10510257
Melatonin regulates glucocorticoid receptor: an answer to its antiapoptotic action in thymus.	1999 Sep	10463946
Morphine induced allodynia in a child with brain tumour.	1999 Sep 4	10473483
Endotoxin-stimulated release of cytokines by cultured cells from the murine neurohypophysis: role of dexamethasone and indomethacin.	1999 Sep-Oct	10474051
Immune abnormalities in aneurysmal subarachnoid haemorrhage patients: relation to delayed cerebral vasospasm.	2000 Apr	10736113
Leptin production in adipocytes from morbidly obese subjects: stimulation by dexamethasone, inhibition with troglitazone, and influence of gender.	2000 Aug	10946865
Dexamethasone-suppressible hypertension.	2000 Aug 26	11085685
Effect of endogenous and exogenous prostaglandin E(2) on interleukin-1 beta-induced cyclooxygenase-2 expression in human airway smooth-muscle cells.	2000 Dec	11112151
Antenatal dexamethasone enhances endothelin receptorB expression in hypoplastic lung in nitrofen-induced diaphragmatic hernia in rats.	2000 Feb	10693666
Dexamethasone differentially regulates expression of carboxylesterase genes in humans and rats.	2000 Feb	10640517
Administration of antenatal glucocorticoids upregulates peptide growth factor gene expression in nitrofen-induced congenital diaphragmatic hernia in rats.	2000 Jan	10646786
Dexamethasone blocks sepsis-induced protection of the heart from ischemia reperfusion injury.	2000 Jan	10632965
Acrylamide-regulated neurofilament expression in rat pheochromocytoma cells.	2000 Jan 10	10678756
Inhibition of carrageenan-induced edema by indomethacin or sodium salicylate does not prevent the increase of nerve growth factor in the rat hind paw.	2000 Jan 14	10653021
Combined administration of G-CSF and dexamethasone for the mobilization of granulocytes in normal donors: optimization of dosing.	2000 Jun	10864982
Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding.	2000 Jun 23	10747884
beta(3)-adrenoceptor regulation and relaxation responses in mouse ileum.	2000 Mar	10725275
Induction and regulation of xenobiotic-metabolizing cytochrome P450s in the human A549 lung adenocarcinoma cell line.	2000 Mar	10696073
Regulation of vitamin D-1alpha-hydroxylase and -24-hydroxylase expression by dexamethasone in mouse kidney.	2000 Mar	10694374
Ticlopidine-induced aplastic anemia: development of chromosomal abnormalities and response to immunosuppressive therapy.	2000 Mar	10679804
Patients with myelodysplastic syndromes benefit from palliative therapy with amifostine, pentoxifylline, and ciprofloxacin with or without dexamethasone.	2000 Mar 1	10688811
Cognitive sequelae in children treated for acute lymphoblastic leukemia with dexamethasone or prednisone.	2000 May-Jun	10864051
Regulation of leptin release by troglitazone in human adipose tissue.	2000 Nov	11092516
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 Oct	11012613
Endotoxin augments cerebral hyperemic response to halothane by inducing nitric oxide synthase and cyclooxygenase.	2000 Oct	11004044
Modification of biophysical properties of lung epithelial Na(+) channels by dexamethasone.	2000 Sep	10942727
Involvement of tyrosine hydroxylase up regulation in dexamethasone-induced hypertension of rats.	2000 Sep 8	11072875
The clinical impact of metabolic bone disease in coeliac disease.	2001 Jan	11123392
Inhibition of NF-kappaB and AP-1 activation by R- and S-flurbiprofen.	2001 Jan	11099482
Topical 0.1% indomethacin solution versus topical 0.1% dexamethasone solution in the prevention of inflammation after cataract surgery. The Study Group.	2001 Jan-Feb	11125269
Triptolide enhances the sensitivity of multiple myeloma cells to dexamethasone via microRNAs.	2012 Jun	22260163
Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity with dexamethasone.	2012 Jun	22207485
CEP-18770 (delanzomib) in combination with dexamethasone and lenalidomide inhibits the growth of multiple myeloma.	2012 Nov	22906694

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.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:46:08 GMT 2025` Edited by `admin` on `Mon Mar 31 17:46:08 GMT 2025`
Record UNII	DWN2WN457X
Record Status	`Validated (UNII)`
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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