Details of the Drug

General Information of Drug (ID: DM8X2EH)

• Drug Name: Everolimus
• Synonyms: Afinitor; Afinitor (TN); CERTICAN(R); Certican; Certican (TN); Everolimus (JAN/USAN/INN); Everolimus [USAN]; MTOR kinase inhibitors; NVP-RAD-001; RAD 001; RAD-001; RAD-001C; RAD001; RAD001, SDZ-RAD, Certican, Zortress, Afinitor, Everolimus; SDZ-RAD; Zortress

Indication

Disease Entry	ICD 11	Status	REF
Advanced cancer	2A00-2F9Z	Approved	[1]
Advanced/metastatic breast cancer	2C60	Approved	[2]
Brainstem neoplasm	N.A.	Approved	[1]
Breast carcinoma	N.A.	Approved	[1]
Graft-versus-host disease	4B24	Approved	[1]
Intracranial meningioma	N.A.	Approved	[1]
Leukemia	N.A.	Approved	[1]
Lung cancer	2C25.0	Approved	[1]
Mucosal melanoma	N.A.	Approved	[1]
Multiple sclerosis	8A40	Approved	[1]
Plasma cell myeloma	2A83.1	Approved	[1]
Prostate cancer	2C82.0	Approved	[1]
Renal cell carcinoma	2C90	Approved	[3]
Salivary gland squamous cell carcinoma	N.A.	Approved	[1]
Tuberous sclerosis	LD2D.2	Approved	[1]
Kidney cancer	2C90.0	Phase 3	[3]
Castration-resistant prostate carcinoma	N.A.	Investigative	[1]
Colon cancer	2B90.Z	Investigative	[1]
Middle East Respiratory Syndrome (MERS)	1D64	Investigative	[4]
Neuroblastoma	2D11.2	Investigative	[1]
Pancreatic acinar cell carcinoma	N.A.	Investigative	[1]
Polycystic kidney disease	GB8Y	Investigative	[1]
Severe acute respiratory syndrome (SARS)	1D65	Investigative	[4]

• Therapeutic Class: Anticancer Agents
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 3:
  Molecular Weight (mw); 958.2
  Logarithm of the Partition Coefficient (xlogp); 5.9
  Rotatable Bond Count (rotbonds); 9
  Hydrogen Bond Donor Count (hbonddonor); 3
  Hydrogen Bond Acceptor Count (hbondacc); 14
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [5]
  Elimination: 0% of drug is excreted from urine in the unchanged form [5]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.1491 micromolar/kg/day [6]
  Water Solubility: The ability of drug to dissolve in water is measured as 0.01 mg/mL [5]
• Chemical Identifiers:
  Formula: C53H83NO14
  IUPAC Name: (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-[(2R)-1-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
  Canonical SMILES: C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)OCCO)C)/C)O)OC)C)C)/C)OC
  InChI: InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-36,38-41,43-46,48-49,55,58,62H,14-15,18-26,28-31H2,1-10H3/b13-11+,16-12+,33-17+,37-27+/t32-,34-,35-,36-,38-,39+,40+,41+,43-,44+,45+,46-,48-,49+,53-/m1/s1
  InChIKey: HKVAMNSJSFKALM-GKUWKFKPSA-N
• Cross-matching ID:
  PubChem CID: 6442177
  ChEBI ID: CHEBI:68478
  CAS Number: 159351-69-6
  DrugBank ID: DB01590
  TTD ID: D0K3QS
  VARIDT ID: DR00224
  INTEDE ID: DR0674
  ACDINA ID: D00260
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Serine/threonine-protein kinase mTOR (mTOR)	TTCJG29	MTOR_HUMAN	Inhibitor	[7]
HUMAN mammalian target of rapamycin (mTOR)	TT7HQAF	MTOR_HUMAN	Inhibitor	[4]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[8]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4) Main DME	DE4LYSA	CP3A4_HUMAN	Substrate	[9]

Molecular Expression Atlas of This Drug

• The Studied Disease: Advanced cancer
• ICD Disease Classification: 2A00-2F9Z

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Serine/threonine-protein kinase mTOR (mTOR)	DTT	MTOR	2.16E-05	-0.44	-2.3
P-glycoprotein 1 (ABCB1)	DTP	P-GP	2.04E-02	-1.13E+00	-1.00E+00
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	5.84E-01	-1.61E-01	-3.61E-01

Drug-Drug Interaction (DDI) Information of This Drug

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

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Remdesivir	DMBFZ6L	Moderate	Decreased renal excretion of Everolimus caused by Remdesivir mediated nephrotoxicity.	1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019]	[10]
Sarecycline	DMLZNIQ	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Sarecycline .	Acne vulgaris [ED80]	[11]
Metreleptin	DM1NOEK	Moderate	Decreased metabolism of Everolimus caused by Metreleptin mediated inhibition of CYP450 enzyme.	Acute diabete complication [5A2Y]	[12]
Ivosidenib	DM8S6T7	Moderate	Increased metabolism of Everolimus caused by Ivosidenib mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[10]
Midostaurin	DMI6E0R	Moderate	Decreased metabolism of Everolimus caused by Midostaurin mediated inhibition of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[11]
Arn-509	DMT81LZ	Major	Increased metabolism of Everolimus caused by Arn-509 mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[13]
Gilteritinib	DMTI0ZO	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Gilteritinib.	Acute myeloid leukaemia [2A60]	[11]
Inotersen	DMJ93CT	Major	Increased risk of nephrotoxicity by the combination of Everolimus and Inotersen.	Amyloidosis [5D00]	[14]
Siltuximab	DMGEATB	Moderate	Additive immunosuppressive effects by the combination of Everolimus and Siltuximab.	Anemia [3A00-3A9Z]	[14]
Dronedarone	DMA8FS5	Major	Decreased metabolism of Everolimus caused by Dronedarone mediated inhibition of CYP450 enzyme.	Angina pectoris [BA40]	[11]
Roflumilast	DMPGHY8	Moderate	Additive immunosuppressive effects by the combination of Everolimus and Roflumilast.	Asthma [CA23]	[14]
Oritavancin	DM28D05	Moderate	Increased metabolism of Everolimus caused by Oritavancin mediated induction of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[10]
Dalfopristin	DM4LTKV	Major	Decreased metabolism of Everolimus caused by Dalfopristin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[11]
Troleandomycin	DMUZNIG	Major	Decreased metabolism of Everolimus caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[10]
Erdafitinib	DMI782S	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Erdafitinib.	Bladder cancer [2C94]	[15]
Pexidartinib	DMS2J0Z	Moderate	Increased metabolism of Everolimus caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[10]
HKI-272	DM6QOVN	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by HKI-272.	Breast cancer [2C60-2C6Y]	[11]
Tucatinib	DMBESUA	Major	Decreased clearance of Everolimus due to the transporter inhibition by Tucatinib.	Breast cancer [2C60-2C6Y]	[10]
Palbociclib	DMD7L94	Moderate	Decreased metabolism of Everolimus caused by Palbociclib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[11]
Iodipamide	DMXIQYS	Major	Increased risk of nephrotoxicity by the combination of Everolimus and Iodipamide.	Cholelithiasis [DC11]	[16]
PF-04449913	DMSB068	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by PF-04449913.	Chronic myelomonocytic leukaemia [2A40]	[11]
Ulipristal	DMBNI20	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Ulipristal.	Contraceptive management [QA21]	[11]
Pasireotide	DMHM7JS	Moderate	Decreased metabolism of Everolimus caused by Pasireotide mediated inhibition of CYP450 enzyme.	Cushing syndrome [5A70]	[11]
Osilodrostat	DMIJC9X	Moderate	Decreased metabolism of Everolimus caused by Osilodrostat mediated inhibition of CYP450 enzyme.	Cushing syndrome [5A70]	[11]
Lumacaftor	DMCLWDJ	Major	Accelerated clearance of Everolimus due to the transporter induction by Lumacaftor.	Cystic fibrosis [CA25]	[13]
Ivacaftor	DMZC1HS	Moderate	Decreased metabolism of Everolimus caused by Ivacaftor mediated inhibition of CYP450 enzyme.	Cystic fibrosis [CA25]	[11]
MK-8228	DMOB58Q	Major	Decreased metabolism of Everolimus caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[11]
Cenobamate	DM8KLU9	Moderate	Increased metabolism of Everolimus caused by Cenobamate mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[10]
Stiripentol	DMMSDOY	Major	Decreased metabolism of Everolimus caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[11]
Rufinamide	DMWE60C	Moderate	Increased metabolism of Everolimus caused by Rufinamide mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[10]
Eslicarbazepine	DMZREFQ	Moderate	Increased metabolism of Everolimus caused by Eslicarbazepine mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[10]
Tazemetostat	DMWP1BH	Moderate	Increased metabolism of Everolimus caused by Tazemetostat mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[10]
Boceprevir	DMBSHMF	Major	Decreased clearance of Everolimus due to the transporter inhibition by Boceprevir.	Hepatitis virus infection [1E50-1E51]	[10]
Simeprevir	DMLUA9D	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Simeprevir.	Hepatitis virus infection [1E50-1E51]	[10]
Telaprevir	DMMRV29	Major	Decreased metabolism of Everolimus caused by Telaprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[10]
Daclatasvir	DMSFK9V	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Daclatasvir.	Hepatitis virus infection [1E50-1E51]	[11]
GS-5885	DMSL3DX	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by GS-5885.	Hepatitis virus infection [1E50-1E51]	[11]
177Lu-DOTATATE	DMT8GVU	Major	Increased risk of nephrotoxicity by the combination of Everolimus and 177Lu-DOTATATE.	Hepatitis virus infection [1E50-1E51]	[17]
Cobicistat	DM6L4H2	Major	Decreased clearance of Everolimus due to the transporter inhibition by Cobicistat.	Human immunodeficiency virus disease [1C60-1C62]	[10]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Everolimus caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[10]
Teriflunomide	DMQ2FKJ	Major	Additive myelosuppressive effects by the combination of Everolimus and Teriflunomide.	Hyper-lipoproteinaemia [5C80]	[18]
BMS-201038	DMQTAGO	Moderate	Decreased metabolism of Everolimus caused by BMS-201038 mediated inhibition of CYP450 enzyme.	Hyper-lipoproteinaemia [5C80]	[11]
Levamlodipine	DM92S6N	Moderate	Decreased metabolism of Everolimus caused by Levamlodipine mediated inhibition of CYP450 enzyme.	Hypertension [BA00-BA04]	[10]
Tolvaptan	DMIWFRL	Moderate	Decreased metabolism of Everolimus caused by Tolvaptan mediated inhibition of CYP450 enzyme.	Hypo-osmolality/hyponatraemia [5C72]	[11]
Givosiran	DM5PFIJ	Major	Increased risk of nephrotoxicity by the combination of Everolimus and Givosiran.	Inborn porphyrin/heme metabolism error [5C58]	[17]
Lesinurad	DMUR64T	Moderate	Increased metabolism of Everolimus caused by Lesinurad mediated induction of CYP450 enzyme.	Inborn purine/pyrimidine/nucleotide metabolism error [5C55]	[19]
Berotralstat	DMWA2DZ	Moderate	Decreased metabolism of Everolimus caused by Berotralstat mediated inhibition of CYP450 enzyme.	Innate/adaptive immunodeficiency [4A00]	[20]
Suvorexant	DM0E6S3	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Suvorexant.	Insomnia [7A00-7A0Z]	[11]
Glycerol phenylbutyrate	DMDGRQO	Moderate	Increased metabolism of Everolimus caused by Glycerol phenylbutyrate mediated induction of CYP450 enzyme.	Liver disease [DB90-DB9Z]	[14]
Denosumab	DMNI0KO	Moderate	Additive myelosuppressive effects by the combination of Everolimus and Denosumab.	Low bone mass disorder [FB83]	[21]
Crizotinib	DM4F29C	Major	Decreased metabolism of Everolimus caused by Crizotinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[11]
Ceritinib	DMB920Z	Major	Decreased clearance of Everolimus due to the transporter inhibition by Ceritinib.	Lung cancer [2C25]	[10]
PF-06463922	DMKM7EW	Moderate	Accelerated clearance of Everolimus due to the transporter induction by PF-06463922.	Lung cancer [2C25]	[10]
Osimertinib	DMRJLAT	Moderate	Increased metabolism of Everolimus caused by Osimertinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[14]
Capmatinib	DMYCXKL	Moderate	Decreased metabolism of Everolimus caused by Capmatinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[11]
Selpercatinib	DMZR15V	Moderate	Decreased metabolism of Everolimus caused by Selpercatinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[11]
Idelalisib	DM602WT	Major	Decreased clearance of Everolimus due to the transporter inhibition by Idelalisib.	Mature B-cell leukaemia [2A82]	[10]
Moxetumomab pasudotox	DMN63DZ	Major	Increased risk of nephrotoxicity by the combination of Everolimus and Moxetumomab pasudotox.	Mature B-cell leukaemia [2A82]	[17]
IPI-145	DMWA24P	Major	Decreased metabolism of Everolimus caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[11]
Blinatumomab	DMGECIJ	Moderate	Decreased metabolism of Everolimus caused by Blinatumomab mediated inhibition of CYP450 enzyme.	Mature B-cell lymphoma [2A85]	[22]
Ibrutinib	DMHZCPO	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Ibrutinib.	Mature B-cell lymphoma [2A85]	[14]
Ponatinib	DMYGJQO	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Ponatinib.	Mature B-cell lymphoma [2A85]	[11]
Vemurafenib	DM62UG5	Moderate	Increased metabolism of Everolimus caused by Vemurafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[10]
LGX818	DMNQXV8	Moderate	Increased metabolism of Everolimus caused by LGX818 mediated induction of CYP450 enzyme.	Melanoma [2C30]	[23]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Everolimus caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[10]
Lasmiditan	DMXLVDT	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Lasmiditan.	Migraine [8A80]	[24]
Gallium nitrate	DMF9O6B	Major	Increased risk of nephrotoxicity by the combination of Everolimus and Gallium nitrate.	Mineral excesses [5B91]	[17]
Flibanserin	DM70DTN	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Flibanserin.	Mood disorder [6A60-6E23]	[11]
Tecfidera	DM2OVDT	Moderate	Additive immunosuppressive effects by the combination of Everolimus and Tecfidera.	Multiple sclerosis [8A40]	[25]
Fingolimod	DM5JVAN	Major	Additive immunosuppressive effects by the combination of Everolimus and Fingolimod.	Multiple sclerosis [8A40]	[26]
Ocrelizumab	DMEZ2KH	Moderate	Additive immunosuppressive effects by the combination of Everolimus and Ocrelizumab.	Multiple sclerosis [8A40]	[27]
Ozanimod	DMT6AM2	Major	Additive immunosuppressive effects by the combination of Everolimus and Ozanimod.	Multiple sclerosis [8A40]	[14]
Fedratinib	DM4ZBK6	Major	Decreased metabolism of Everolimus caused by Fedratinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[11]
Nilotinib	DM7HXWT	Moderate	Decreased metabolism of Everolimus caused by Nilotinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[11]
Omacetaxine mepesuccinate	DMPU2WX	Moderate	Additive immunosuppressive effects by the combination of Everolimus and Omacetaxine mepesuccinate.	Myeloproliferative neoplasm [2A20]	[28]
Rolapitant	DM8XP26	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Rolapitant.	Nausea/vomiting [MD90]	[29]
Netupitant	DMEKAYI	Major	Decreased clearance of Everolimus due to the transporter inhibition by Netupitant.	Nausea/vomiting [MD90]	[11]
Entrectinib	DMMPTLH	Moderate	Decreased metabolism of Everolimus caused by Entrectinib mediated inhibition of CYP450 enzyme.	Non-small cell lung cancer [2C25]	[11]
Rucaparib	DM9PVX8	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Rucaparib.	Ovarian cancer [2C73]	[11]
Istradefylline	DM20VSK	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Istradefylline.	Parkinsonism [8A00]	[11]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Everolimus caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[30]
Lanreotide acetate	DMG6ZU4	Moderate	Decreased metabolism of Everolimus caused by Lanreotide acetate mediated inhibition of CYP450 enzyme.	Pituitary gland disorder [5A60-5A61]	[11]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Everolimus caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[31]
Lonafarnib	DMGM2Z6	Major	Decreased metabolism of Everolimus caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[10]
ABIRATERONE	DM8V75C	Moderate	Decreased metabolism of Everolimus caused by ABIRATERONE mediated inhibition of CYP450 enzyme.	Prostate cancer [2C82]	[11]
Enzalutamide	DMGL19D	Major	Increased metabolism of Everolimus caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[13]
Ustekinumab	DMHTYK3	Moderate	Additive immunosuppressive effects by the combination of Everolimus and Ustekinumab.	Psoriasis [EA90]	[14]
Tildrakizumab	DMLW9HG	Moderate	Additive myelosuppressive effects by the combination of Everolimus and Tildrakizumab.	Psoriasis [EA90]	[14]
Risankizumab	DMM32GT	Moderate	Additive myelosuppressive effects by the combination of Everolimus and Risankizumab.	Psoriasis [EA90]	[14]
Ixekizumab	DMXW92T	Moderate	Additive myelosuppressive effects by the combination of Everolimus and Ixekizumab.	Psoriasis [EA90]	[14]
Tocilizumab	DM7J6OR	Moderate	Additive immunosuppressive effects by the combination of Everolimus and Tocilizumab.	Rheumatoid arthritis [FA20]	[14]
Canakinumab	DM8HLO5	Moderate	Additive immunosuppressive effects by the combination of Everolimus and Canakinumab.	Rheumatoid arthritis [FA20]	[14]
Rilonacept	DMGLUQS	Moderate	Additive myelosuppressive effects by the combination of Everolimus and Rilonacept.	Rheumatoid arthritis [FA20]	[14]
Golimumab	DMHZV7X	Major	Additive immunosuppressive effects by the combination of Everolimus and Golimumab.	Rheumatoid arthritis [FA20]	[32]
Sarilumab	DMOGNXY	Moderate	Additive immunosuppressive effects by the combination of Everolimus and Sarilumab.	Rheumatoid arthritis [FA20]	[14]
Anthrax vaccine	DM9GSWY	Moderate	Antagonize the effect of Everolimus when combined with Anthrax vaccine.	Sepsis [1G40-1G41]	[33]
Voxelotor	DMCS6M5	Major	Decreased metabolism of Everolimus caused by Voxelotor mediated inhibition of CYP450 enzyme.	Sickle-cell disorder [3A51]	[11]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Everolimus caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[14]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Everolimus caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[11]
Armodafinil	DMGB035	Moderate	Increased metabolism of Everolimus caused by Armodafinil mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[10]
LEE011	DMMX75K	Major	Decreased metabolism of Everolimus caused by LEE011 mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[11]
Telavancin	DM58VQX	Major	Increased risk of nephrotoxicity by the combination of Everolimus and Telavancin.	Staphylococcal/streptococcal disease [1B5Y]	[17]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Everolimus caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[34]
Brilinta	DMBR01X	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Brilinta.	Thrombosis [DB61-GB90]	[11]
Cabozantinib	DMIYDT4	Moderate	Decreased clearance of Everolimus due to the transporter inhibition by Cabozantinib.	Thyroid cancer [2D10]	[11]
Plazomicin	DMKMBES	Major	Increased risk of nephrotoxicity by the combination of Everolimus and Plazomicin.	Urinary tract infection [GC08]	[17]
Elagolix	DMB2C0E	Moderate	Increased metabolism of Everolimus caused by Elagolix mediated induction of CYP450 enzyme.	Uterine fibroid [2E86]	[10]

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
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Crospovidone	E00626	Not Available	Disintegrant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Everolimus 2 mg tablet	2 mg	Tablet for Oral Suspension	Oral
Everolimus 3 mg tablet	3 mg	Tablet for Oral Suspension	Oral
Everolimus 5 mg tablet	5 mg	Tablet for Oral Suspension	Oral
Everolimus 0.25 mg tablet	0.25 mg	Oral Tablet	Oral
Everolimus 0.5 mg tablet	0.5 mg	Oral Tablet	Oral
Everolimus 0.75 mg tablet	0.75 mg	Oral Tablet	Oral
Everolimus 10 mg tablet	10 mg	Oral Tablet	Oral
Everolimus 2.5 mg tablet	2.5 mg	Oral Tablet	Oral
Everolimus 5 mg tablet	5 mg	Oral Tablet	Oral
Everolimus 7.5 mg tablet	7.5 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] Everolimus FDA Label
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [3] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5889).
• [4] Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47.
• [5] BDDCS applied to over 900 drugs
• [6] Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
• [7] Mammalian target of rapamycin, its mode of action and clinical response in metastatic clear cell carcinoma. Gan To Kagaku Ryoho. 2009 Jul;36(7):1076-9.
• [8] Closer to the Site of Action: Everolimus Concentrations in Peripheral Blood Mononuclear Cells Correlate Well With Whole Blood Concentrations. Ther Drug Monit. 2015 Oct;37(5):675-80.
• [9] The evolving experience using everolimus in clinical transplantation. Transplant Proc. 2004 Mar;36(2 Suppl):495S-499S.
• [10] Cerner Multum, Inc. "Australian Product Information.".
• [11] Product Information. Afinitor (everolimus). Novartis Pharmaceuticals, East Hanover, NJ.
• [12] Product Information. Myalept (metreleptin). Bristol-Myers Squibb, Princeton, NJ.
• [13] Canadian Pharmacists Association.
• [14] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [15] Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
• [16] Wong GT, Lee EY, Irwin MG. Contrast induced nephropathy in vascular surgery.?Br J Anaesth. 2016;117 Suppl 2:ii63-ii73. [PMID: 27566809]
• [17] Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
• [18] Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
• [19] Product Information. Zurampic (lesinurad). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
• [20] Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
• [21] Product Information. Prolia (denosumab). Amgen USA, Thousand Oaks, CA.
• [22] Product Information. Blincyto (blinatumomab). Amgen USA, Thousand Oaks, CA.
• [23] Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
• [24] Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
• [25] Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA.
• [26] Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
• [27] Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
• [28] Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
• [29] Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
• [30] Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
• [31] Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
• [32] Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA.
• [33] CDC. Centers for Disease Control and Prevention/ "Recommendations of the advisory committtee on immunization practices (ACIP): use of vaccines and immune globulins in persons with altered immunocompetence." MMWR Morb Mortal Wkly Rep 42(RR-04) (1993): 1-18. [PMID: 20300058]
• [34] Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.