Details of the Drug

General Information of Drug (ID: DM9HPW3)

Drug Name

Exemestane

Synonyms

Aromasil; Aromasin; Aromasine; EXE; Exemestance; Exemestano; Exemestanum; Nikidess; Pfizer brand of exemestane; Curator_000009; Fce 24304; Aromasin (TN); Aromasin, Exemestane; Exemestano [INN-Spanish]; Exemestanum [INN-Latin]; FCE-24304; PNU-155971; Exemestane [USAN:INN:BAN]; Exemestane (JAN/USP/INN); (8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylidene-7,8,9,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-3,17-dione; 6-Methylenandrosta-1,4-diene-3,17-dione; 6-Methyleneandrosta-1,4-diene-3,17-dione; 6-methylideneandrosta-1,4-diene-3,17-dione

Indication

Disease Entry	ICD 11	Status	REF
Hormonally-responsive breast cancer	2C60-2C65	Approved	[1], [2]

Therapeutic Class

Anticancer Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

296.4

Topological Polar Surface Area (xlogp)

3.1

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption: The absorption of drug is 42% [3]
BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Elimination: 1% of drug is excreted from urine in the unchanged form [4]
Half-life: The concentration or amount of drug in body reduced by one-half in 24 hours [5]
Metabolism: The drug is metabolized via the hepatic [3]
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.34947 micromolar/kg/day [6]

Chemical Identifiers

Formula: C20H24O2
IUPAC Name: (8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylidene-7,8,9,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-3,17-dione
Canonical SMILES: C[C@]12CC[C@H]3[C@H]([C@@H]1CCC2=O)CC(=C)C4=CC(=O)C=C[C@]34C
InChI: InChI=1S/C20H24O2/c1-12-10-14-15-4-5-18(22)20(15,3)9-7-16(14)19(2)8-6-13(21)11-17(12)19/h6,8,11,14-16H,1,4-5,7,9-10H2,2-3H3/t14-,15-,16-,19+,20-/m0/s1
InChIKey: BFYIZQONLCFLEV-DAELLWKTSA-N

Cross-matching ID

PubChem CID: 60198
ChEBI ID: CHEBI:4953
CAS Number: 107868-30-4
DrugBank ID: DB00990
TTD ID: D0D2VS
INTEDE ID: DR0675
ACDINA ID: D00261

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Aromatase (CYP19A1)	TTSZLWK	CP19A_HUMAN	Inhibitor	[7]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)_{Main DME}	DE4LYSA	CP3A4_HUMAN	Substrate	[8]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Exemestane (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Ivosidenib	DM8S6T7	Moderate	Increased metabolism of Exemestane caused by Ivosidenib mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[27]
Arn-509	DMT81LZ	Moderate	Increased metabolism of Exemestane caused by Arn-509 mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[27]
Pexidartinib	DMS2J0Z	Moderate	Increased metabolism of Exemestane caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[27]
Lumacaftor	DMCLWDJ	Moderate	Increased metabolism of Exemestane caused by Lumacaftor mediated induction of CYP450 enzyme.	Cystic fibrosis [CA25]	[28]
Cenobamate	DMGOVHA	Moderate	Increased metabolism of Exemestane caused by Cenobamate mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[27]
Fosphenytoin	DMOX3LB	Moderate	Increased metabolism of Exemestane caused by Fosphenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[27]
Rufinamide	DMWE60C	Moderate	Increased metabolism of Exemestane caused by Rufinamide mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[29]
Phenobarbital	DMXZOCG	Moderate	Increased metabolism of Exemestane caused by Phenobarbital mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[27]
Eslicarbazepine	DMZREFQ	Moderate	Increased metabolism of Exemestane caused by Eslicarbazepine mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[27]
Tazemetostat	DMWP1BH	Moderate	Increased metabolism of Exemestane caused by Tazemetostat mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[27]
Sulfinpyrazone	DMEV954	Moderate	Increased metabolism of Exemestane caused by Sulfinpyrazone mediated induction of CYP450 enzyme.	Gout [FA25]	[27]
Rifampin	DMA8J1G	Moderate	Increased metabolism of Exemestane caused by Rifampin mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[28]
Rifapentine	DMCHV4I	Moderate	Increased metabolism of Exemestane caused by Rifapentine mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[27]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Exemestane caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[27]
Amobarbital	DM0GQ8N	Moderate	Increased metabolism of Exemestane caused by Amobarbital mediated induction of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[27]
Brigatinib	DM7W94S	Moderate	Increased metabolism of Exemestane caused by Brigatinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[30]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Exemestane caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[27]
Vemurafenib	DM62UG5	Moderate	Increased metabolism of Exemestane caused by Vemurafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[27]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Exemestane caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[27]
Exjade	DMHPRWG	Moderate	Decreased metabolism of Exemestane caused by Exjade mediated inhibition of CYP450 enzyme.	Mineral absorption/transport disorder [5C64]	[31]
Thalidomide	DM70BU5	Major	Additive thrombogenic effects by the combination of Exemestane and Thalidomide.	Multiple myeloma [2A83]	[32]
Omacetaxine mepesuccinate	DMPU2WX	Moderate	Additive myelosuppressive effects by the combination of Exemestane and Omacetaxine mepesuccinate.	Myeloproliferative neoplasm [2A20]	[33]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Exemestane caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[34]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Exemestane caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[35]
Enzalutamide	DMGL19D	Moderate	Increased metabolism of Exemestane caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[27]
Temsirolimus	DMS104F	Moderate	Increased plasma concentrations of Exemestane and Temsirolimus due to competitive inhibition of the same metabolic pathway.	Renal cell carcinoma [2C90]	[36]
Dexamethasone	DMMWZET	Moderate	Increased metabolism of Exemestane caused by Dexamethasone mediated induction of CYP450 enzyme.	Rheumatoid arthritis [FA20]	[27]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Exemestane caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[29]
Armodafinil	DMGB035	Moderate	Increased metabolism of Exemestane caused by Armodafinil mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[27]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Exemestane caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[37]
Elagolix	DMB2C0E	Moderate	Increased metabolism of Exemestane caused by Elagolix mediated induction of CYP450 enzyme.	Uterine fibroid [2E86]	[27]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Butylated hydroxytoluene	E00336	31404	Antioxidant
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
methylparaben	E00149	7456	Antimicrobial preservative
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Butylhydroxyanisole	E00308	24667	Antimicrobial preservative; Antioxidant
Crospovidone	E00626	Not Available	Disintegrant
Hypromellose	E00634	Not Available	Coating agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium carbonate	E00205	11029	Adsorbent; Diluent
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 6000	E00655	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Polyvinyl alcohol	E00666	Not Available	Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Saccharose	E00091	5988	Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium bicarbonate	E00424	516892	Alkalizing agent; Diluent
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Triacetin	E00080	5541	Humectant; Plasticizing agent; Solvent
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⏷ Show the Full List of 18 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Exemestane 25 mg tablet	25 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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27	Product Information. Aromasin (exemestane) Pharmacia & Upjohn, Kalamazoo, MI.
28	Product Information. Aromasin (exemestane) Pharmacia &amp Upjohn, Kalamazoo, MI.
29	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
30	Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
31	Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
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33	Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
34	Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
35	Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ.
36	Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
37	Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.