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Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:03:52
Primary Accession Number DB00976
Secondary Accession Number
  • APRD00483
Name Telithromycin
Drug Type
  • Approved
  • Investigational
  • Small Molecule
Description Telithromycin is a semi-synthetic erythromycin derivative. It is used to treat mild to moderate respiratory infections. Telithromycin prevents bacteria from growing, by interfering with their protein synthesis. Telithromycin binds to the subunit 50S of the bacterial ribosome, and blocks the progression of the growing polypeptide chain. In addition, telithromycin binds simultaneously to two domains of 23S RNA of the 50 S ribosomal subunit, where older macrolides bind only to one.
Synonyms
  1. telithromycin
Brand Names
  1. Ketek
Brand Mixtures Not Available
Chemical IUPAC Name (1R,2R,4R,6S,7R,8R,10R,13R,14S)-7-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-13-ethyl-6-methoxy-2,4,6,8,10,14-hexamethyl-17-[4-(4-pyridin-3-ylimidazol-1-yl)butyl]-12,15-dioxa-17-azabicyclo[12.3.0]heptadecane-3,9,11,16-tetrone
Chemical Formula C43H65N5O10
Chemical Structure Structure
CAS Registry Number 191114-48-4
InChI Identifier InChI=1/C43H65N5O10/c1-12-33-43(8)37(48(41(53)58-43)19-14-13-18-47-23-31(45-24-47)30-16-15-17-44-22-30)27(4)34(49)25(2)21-42(7,54-11)38(28(5)35(50)29(6)39(52)56-33)57-40-36(51)32(46(9)10)20-26(3)55-40/h15-17,22-29,32-33,36-38,40,51H,12-14,18-21H2,1-11H3/t25-,26-,27-,28+,29-,32+,33+,36-,37-,38-,40+,42+,43-/m1/s1
InChI Key LJVAJPDWBABPEJ-WIFJXVANBD
KEGG Drug D01078 Link Image
KEGG Compound C12009 Link Image
PubChem Compound 5462516 Link Image
PubChem Substance 14168 Link Image
ChEBI ID Not Available
PharmGKB ID PA10202 Link Image
HET ID TEL Link Image
GenBank ID Not Available
Drug ID Number [DIN] 02247520 Link Image
RxList Link http://www.rxlist.com/cgi/generic3/ketek.htm Link Image
PDRhealth Link http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ket1695.shtml Link Image
Wikipedia Link http://en.wikipedia.org/wiki/Telithromycin Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 812.0037
Monoisotopic Molecular Weight 811.4731
State Solid
Melting Point 176-188 oC
Experimental Water Solubility 300 mg/L Source: PhysProp
Predicted Water Solubility 2.83e-02 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 3 Source: PhysProp
Predicted LogP 4.01 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -4.46 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES CC[C@@H]1OC(=O)[C@H](C)C(=O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)C)[C@](C)(C[C@@H](C)C(=O)[C@@H](C)[C@H]2N(CCCCN3C=NC(=C3)C3=CN=CC=C3)C(=O)O[C@]12C)OC
Canonical SMILES CCC1OC(=O)C(C)C(=O)C(C)C(OC2OC(C)CC(C2O)N(C)C)C(C)(CC(C)C(=O)C(C)C2N(CCCCN3C=NC(=C3)C3=CN=CC=C3)C(=O)OC12C)OC
Drug Category
  • Anti-Bacterial Agents
  • Ketolides
ATC Codes
AHFS Codes
  • 08:12.12.12
Indication For the treatment of Pneumococcal infection, acute sinusitis, acute bacterial tonsillitis, acute bronchitis and bronchiolitis, lower respiratory tract infection and lobar (pneumococcal) pneumonia.
Pharmacology Telithromycin is a macrolide antibiotic which has an antimicrobial spectrum similar or slightly wider to that of penicillin, and is often used for people who have an allergy to penicillins. For respiratory tract infections, it has better coverage of atypical organisms, including mycoplasma. It is also used to treat outbreaks of chlamydia, syphilis, and gonorrhea. Telithromycin prevents bacteria from growing, by interfering with their protein synthesis. Telithromycin binds to the subunit 50S of the bacterial ribosome, and thus inhibits the translocation of peptides.
Mechanism of Action Telithromycin acts by binding to domains II and V of 23S rRNA of the 50S ribosomal subunit. By binding at domain II, telithromycin retains activity against gram-positive cocci (e.g., Streptococcus pneumoniae) in the presence of resistance mediated by methylases (erm genes) that alter the domain V binding site of telithromycin. Telithromycin may also inhibit the assembly of nascent ribosomal units.
Absorption Not Available
Toxicity LD50>2000 mg/kg (PO in rats)
Protein Binding 60%-70%
Biotransformation Hepatic
Half Life 10 hours
Dosage Forms
Form Route
Tablet Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Acenocoumarol Telithromycin increases the anticoagulant effect
Alfentanil Telithromycin may reduce clearance of Alfentanil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Alfentanil if Telithromycin is initiated, discontinued or dose changed.
Alfuzosin Telithromycin may reduce clearance of Alfuzosin. Consider alternate therapy.
Alprazolam Telithromycin increases the effect/toxicity of the benzodiazepine
Alprazolam Telithromycin may reduce clearance of Alprazolam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Alprazolam if Telithromycin is initiated, discontinued or dose changed.
Aminoglutethimide Aminoglutethimide may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Amiodarone Increased risk of cardiotoxicity and arrhythmias
Amiodarone Telithromycin may reduce clearance of Amiodarone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Amiodarone if Telithromycin is initiated, discontinued or dose changed.
Amlodipine Telithromycin may reduce clearance of Amlopidine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Amlopidine if Telithromycin is initiated, discontinued or dose changed.
Amprenavir Co-administration may result in altered plasma concentrations of Amprenavir and/or Telithromycin. Consider alternate therapy or monitor the therapeutic/adverse effects of both agents.
Anisindione Telithromycin increases the anticoagulant effect
Aprepitant Telithromycin may reduce clearance of Aprepitant. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Aprepitant if Telithromycin is initiated, discontinued or dose changed.
Aripiprazole Telithromycin may reduce clearance of Aripiprazole. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Aripiprazole if Telithromycin is initiated, discontinued or dose changed.
Astemizole Increased risk of cardiotoxicity and arrhythmias
Atazanavir Co-administration may result in altered plasma concentrations of Atazanavir and/or Telithromycin. Consider alternate therapy or monitor the therapeutic/adverse effects of both agents.
Atorvastatin Telithromycin may possibly increase statin toxicity
Atorvastatin Telithromycin may reduce clearance of Atorvastatin. Concomitant therapy is contraindicated.
Benzphetamine Telithromycin may reduce clearance of Benzphetamine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Benzphetamine if Telithromycin is initiated, discontinued or dose changed.
Bisoprolol Telithromycin may reduce clearance of Bisoprolol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Bisoprolol if Telithromycin is initiated, discontinued or dose changed.
Bortezomib Telithromycin may reduce clearance of Bortezomib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Bortezomib if Telithromycin is initiated, discontinued or dose changed.
Bosentan Co-administration may cause decreased Telithromycin and increased Bosentan plasma concentrations. Consider alternate therapy.
Bretylium Increased risk of cardiotoxicity and arrhythmias
Bromazepam Telithromycin may reduce clearance of Bromazepam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Bromazepam if Telithromycin is initiated, discontinued or dose changed.
Bromocriptine Telithromycin may reduce clearance of Bromocriptine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Bromocriptine if Telithromycin is initiated, discontinued or dose changed.
Budesonide Telithromycin may reduce clearance of Budesonide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Budesonide if Telithromycin is initiated, discontinued or dose changed.
Buprenorphine Telithromycin may reduce clearance of Buprenorphine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Buprenorphine if Telithromycin is initiated, discontinued or dose changed.
Buspirone Telithromycin may reduce clearance of Buspirone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Buspirone if Telithromycin is initiated, discontinued or dose changed.
Busulfan Telithromycin may reduce clearance of Busulfan. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Busulfan if Telithromycin is initiated, discontinued or dose changed.
Calcitriol Telithromycin may reduce clearance of Calcitriol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Calcitriol if Telithromycin is initiated, discontinued or dose changed.
Carbamazepine Co-administration may cause decreased Telithromycin and increased Carbemazepine plasma concentrations. Consider alternate therapy.
Carbamazepine Telithromycin may possibly increase this agent effect/toxicity
Chlordiazepoxide Telithromycin may reduce clearance of Chlordiazepoxide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Chlordiazepoxide if Telithromycin is initiated, discontinued or dose changed.
Chloroquine Telithromycin may reduce clearance of Chloroquine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Chloroquine if Telithromycin is initiated, discontinued or dose changed.
Chlorpheniramine Telithromycin may reduce clearance of Chlorpheniramine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Chlorpheniramine if Telithromycin is initiated, discontinued or dose changed.
Ciclesonide Telithromycin may reduce clearance of Ciclesonide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ciclesonide if Telithromycin is initiated, discontinued or dose changed.
Cilostazol Telithromycin may reduce clearance of Cilostazol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Cilostazol if Telithromycin is initiated, discontinued or dose changed.
Cinacalcet Telithromycin may reduce clearance of Cinacalcet. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Cinacalcet if Telithromycin is initiated, discontinued or dose changed.
Cisapride Increased risk of cardiotoxicity and arrhythmias
Cisapride Telithromycin may reduce clearance of Cisapride. Concomitant therapy is contraindicated.
Citalopram Telithromycin may reduce clearance of Citalopram. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Citalopram if Telithromycin is initiated, discontinued or dose changed.
Clarithromycin Co-administration may result in altered plasma concentrations of Clarithromycin and/or Telithromycin. Consider alternate therapy or monitor the therapeutic/adverse effects of both agents.
Clobazam Telithromycin may reduce clearance of Clobazam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Clobazam if Telithromycin is initiated, discontinued or dose changed.
Clonazepam Telithromycin may reduce clearance of Clonazepam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Clonazepam if Telithromycin is initiated, discontinued or dose changed.
Clorazepate Telithromycin may reduce clearance of Clorazepate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Clorazepate if Telithromycin is initiated, discontinued or dose changed.
Cocaine Telithromycin may reduce clearance of Cocaine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Cocaine if Telithromycin is initiated, discontinued or dose changed.
Colchicine Severe colchicine toxicity can occur
Colchicine Telithromycin may reduce clearance of Colchicine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Colchicine if Telithromycin is initiated, discontinued or dose changed.
Conivaptan Co-administration may result in altered plasma concentrations of Conivaptan and/or Telithromycin. Consider alternate therapy or monitor the therapeutic/adverse effects of both agents.
Cyclosporine Telithromycin may possibly increase this agent effect/toxicity
Cyclosporine Telithromycin may reduce clearance of Cyclosporine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Cyclosporine if Telithromycin is initiated, discontinued or dose changed.
Dantrolene Telithromycin may reduce clearance of Dantrolene. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Dantrolene if Telithromycin is initiated, discontinued or dose changed.
Dapsone Telithromycin may reduce clearance of Dapsone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Dapsone if Telithromycin is initiated, discontinued or dose changed.
Darifenacin Telithromycin may reduce clearance of Darifenacin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Darifenacin if Telithromycin is initiated, discontinued or dose changed.
Darunavir Co-administration may result in altered plasma concentrations of Darunavir and/or Telithromycin. Consider alternate therapy or monitor the therapeutic/adverse effects of both agents.
Dasatinib Increased levels/toxicity of dasatinib
Dasatinib Telithromycin may reduce clearance of Dasatinib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Dasatinib if Telithromycin is initiated, discontinued or dose changed.
Delavirdine Delavirdine may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Dexamethasone Co-administration may cause decreased Telithromycin and increased Dexamethasone plasma concentrations. Consider alternate therapy.
Diazepam Telithromycin may reduce clearance of Diazepam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Diazepam if Telithromycin is initiated, discontinued or dose changed.
Dicumarol Telithromycin increases the anticoagulant effect
Digitoxin Telithromycin may reduce clearance of Digitoxin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Digitoxin if Telithromycin is initiated, discontinued or dose changed.
Digoxin Telithromycin may increase levels of digoxin
Digoxin Telithromycin may increase the plasma concentration of Digoxin. Monitor for changes in Digoxin efficacy/toxicity if Telithromycin is initiated, discontinued or dose changed.
Dihydroergotamine Risk of ergotism and severe ischemia with this association
Dihydroergotamine Telithromycin may reduce clearance of Dihydroergotamine. Concomitant therapy is contraindicated.
Diltiazem Telithromycin may reduce clearance of Diltiazem. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Diltiazem if Telithromycin is initiated, discontinued or dose changed.
Disopyramide Increased risk of cardiotoxicity and arrhythmias
Disopyramide Telithromycin may reduce clearance of Disopyramide. Concomitant therapy should be avoided.
Docetaxel Telithromycin may reduce clearance of Docetaxel. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Docetaxel if Telithromycin is initiated, discontinued or dose changed.
Dofetilide Increased risk of cardiotoxicity and arrhythmias
Doxepin Telithromycin may reduce clearance of Doxepin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Doxepin if Telithromycin is initiated, discontinued or dose changed.
Doxorubicin Telithromycin may reduce clearance of Doxorubicin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Doxorubicin if Telithromycin is initiated, discontinued or dose changed.
Efavirenz Efavirenz may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Eletriptan Telithromycin may reduce clearance of Eletriptan. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Eletriptan if Telithromycin is initiated, discontinued or dose changed.
Eplerenone Telithromycin may reduce clearance of Eplerenone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Eplerenone if Telithromycin is initiated, discontinued or dose changed.
Ergoloid mesylate Telithromycin may reduce clearance of Ergoloid mesylates. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ergoloid mesylates if Telithromycin is initiated, discontinued or dose changed.
Ergonovine Telithromycin may reduce clearance of Ergonovine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ergonivine if Telithromycin is initiated, discontinued or dose changed.
Ergotamine Risk of ergotism and severe ischemia with this association
Ergotamine Telithromycin may reduce clearance of Ergotamine. Concomitant therapy is contraindicated.
Erlotinib Telithromycin may reduce clearance of Erlotinib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Erlotinib if Telithromycin is initiated, discontinued or dose changed.
Erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib
Erythromycin Telithromycin may reduce clearance of Erythromycin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Erythromycin if Telithromycin is initiated, discontinued or dose changed.
Escitalopram Telithromycin may reduce clearance of Escitalopram. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Escitalopram if Telithromycin is initiated, discontinued or dose changed.
Eszopiclone Telithromycin may reduce clearance of Eszopiclone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Eszopiclone if Telithromycin is initiated, discontinued or dose changed.
Ethosuximide Telithromycin may reduce clearance of Ethosuximide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ethosuximide if Telithromycin is initiated, discontinued or dose changed.
Etoposide Telithromycin may reduce clearance of Etoposide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Etoposide if Telithromycin is initiated, discontinued or dose changed.
Felbamate Telithromycin may reduce clearance of Felbamate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Felbamate if Telithromycin is initiated, discontinued or dose changed.
Felodipine Telithromycin may reduce clearance of Felodipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Felodipine if Telithromycin is initiated, discontinued or dose changed.
Fentanyl Telithromycin may reduce clearance of Fentanyl. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Fentanyl if Telithromycin is initiated, discontinued or dose changed.
Flunisolide Telithromycin may reduce clearance of Flunisolide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Flunisolide if Telithromycin is initiated, discontinued or dose changed.
Flurazepam Telithromycin may reduce clearance of Flurazepam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Flurazepam if Telithromycin is initiated, discontinued or dose changed.
Flutamide Telithromycin may reduce clearance of Flutamide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Flutamide if Telithromycin is initiated, discontinued or dose changed.
Fluticasone Propionate Telithromycin may reduce clearance of Fluticasone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Fluticasone if Telithromycin is initiated, discontinued or dose changed.
Fosamprenavir Fosamprevavir may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Fosphenytoin Fosphenytoin may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Fosphenytoin Telithromycin may possibly increase this agent effect/toxicity
Gefitinib Telithromycin may reduce clearance of Gefitinib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Gefitinib if Telithromycin is initiated, discontinued or dose changed.
Halofantrine Telithromycin may reduce clearance of Halofantrine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Halofantrine if Telithromycin is initiated, discontinued or dose changed.
Haloperidol Telithromycin may reduce clearance of Haloperidol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Haloperidol if Telithromycin is initiated, discontinued or dose changed.
Ifosfamide Telithromycin may reduce clearance of Ifosfamide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ifosfamide if Telithromycin is initiated, discontinued or dose changed.
Imatinib Co-administration may result in altered plasma concentrations of Imatinib and/or Telithromycin. Consider alternate therapy or monitor the therapeutic/adverse effects of both agents.
Indinavir Indinavir may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Irinotecan Telithromycin may reduce clearance of Irinotecan. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Irinotecan if Telithromycin is initiated, discontinued or dose changed.
Isoniazid Isoniazid may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Isosorbide Dinitrate Telithromycin may reduce clearance of Isosorbide Dinitrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Isosorbide Dinitrate if Telithromycin is initiated, discontinued or dose changed.
Isosorbide Mononitrate Telithromycin may reduce clearance of Isosorbide Mononitrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Isosorbide Mononitrate if Telithromycin is initiated, discontinued or dose changed.
Isradipine Telithromycin may reduce clearance of Isradipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Isradipine if Telithromycin is initiated, discontinued or dose changed.
Itraconazole Itraconazole may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Ixabepilone Telithromycin may reduce clearance of Ixabepilone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ixabepilone if Telithromycin is initiated, discontinued or dose changed.
Ketamine Telithromycin may reduce clearance of Ketamine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ketamine if Telithromycin is initiated, discontinued or dose changed.
Ketoconazole Ketoconazole may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Lapatinib Telithromycin may reduce clearance of Lapatinib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Lapatinib if Telithromycin is initiated, discontinued or dose changed.
Lidocaine Telithromycin may reduce clearance of Lidocaine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Lidocaine if Telithromycin is initiated, discontinued or dose changed.
Lopinavir Lopinavir may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Lovastatin Telithromycin may possibly increase statin toxicity
Lovastatin Telithromycin may reduce clearance of Lovastatin. Concomitant therapy is contraindicated.
Maraviroc Telithromycin may reduce clearance of Maraviroc. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Maraviroc if Telithromycin is initiated, discontinued or dose changed.
Mefloquine Telithromycin may reduce clearance of Mefloquine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Mefloquine if Telithromycin is initiated, discontinued or dose changed.
Methadone Telithromycin may reduce clearance of Methadone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Methadone if Telithromycin is initiated, discontinued or dose changed.
Methylergonovine Telithromycin may reduce clearance of Methylergonovine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Methylergonovine if Telithromycin is initiated, discontinued or dose changed.
Methysergide Risk of ergotism and severe ischemia with this association
Metoprolol Telithromycin may increase the concentration Metoprolol.
Metoprolol Telithromycin may possibly increase metoprolol effect
Miconazole Miconazole may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Midazolam Telithromycin increases the effect/toxicity of the benzodiazepine
Midazolam Telithromycin may reduce clearance of Midazolam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Midazolam if Telithromycin is initiated, discontinued or dose changed.
Mirtazapine Telithromycin may reduce clearance of Mirtazapine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Mirtazapine if Telithromycin is initiated, discontinued or dose changed.
Modafinil Telithromycin may reduce clearance of Modafinil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Modafinil if Telithromycin is initiated, discontinued or dose changed.
Moricizine Telithromycin may reduce clearance of Moricizine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Moricizine if Telithromycin is initiated, discontinued or dose changed.
Nafcillin Nafcillin may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Nateglinide Telithromycin may reduce clearance of Nateglenide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nateglenide if Telithromycin is initiated, discontinued or dose changed.
Nefazodone Co-administration may result in altered plasma concentrations of Nefazodone and/or Telithromycin. Consider alternate therapy or monitor the therapeutic/adverse effects of both agents.
Nelfinavir Nelfinavir may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Nevirapine Nevirapine may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Nicardipine Co-administration may result in altered plasma concentrations of Nicardipine and/or Telithromycin. Consider alternate therapy or monitor the therapeutic/adverse effects of both agents.
Nifedipine Telithromycin may reduce clearance of Nifedipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nifedipine if Telithromycin is initiated, discontinued or dose changed.
Nilotinib Telithromycin may reduce clearance of Nilotinib. Concomitant therapy should be avoided.
Nilotinib This CYP3A4 inhibitor increases the level of nilotinib
Nimodipine Telithromycin may reduce clearance of Nimodipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nimodipine if Telithromycin is initiated, discontinued or dose changed.
Nisoldipine Telithromycin may reduce clearance of Nisoldipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nisoldipine if Telithromycin is initiated, discontinued or dose changed.
Nitrendipine Telithromycin may reduce clearance of Nitrendipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nitrendipine if Telithromycin is initiated, discontinued or dose changed.
Oxcarbazepine Oxcarbazepine may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Paclitaxel Telithromycin may reduce clearance of Paclitaxel. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Paclitaxel if Telithromycin is initiated, discontinued or dose changed.
Pentobarbital Pentobarbital may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Pergolide Telithromycin may reduce clearance of Pergolide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Pergolide if Telithromycin is initiated, discontinued or dose changed.
Phencyclidine Telithromycin may reduce clearance of Phencyclidine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Phencyclidine if Telithromycin is initiated, discontinued or dose changed.
Phenobarbital Phenobarbital may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Phenytoin Phenytoin may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Phenytoin Telithromycin may possibly increase this agent effect/toxicity
Pimozide Increased risk of cardiotoxicity and arrhythmias
Pimozide Telithromycin may reduce clearance of Pimozide. Concomitant therapy is contraindicated.
Pipotiazine Telithromycin may reduce clearance of Pipotiazine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Pipotiazine if Telithromycin is initiated, discontinued or dose changed.
Posaconazole Posaconazole may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Praziquantel Telithromycin may reduce clearance of Praziquantel. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Praziquantel if Telithromycin is initiated, discontinued or dose changed.
Primidone Primidone may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Quetiapine Telithromycin may reduce clearance of Quetiapine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Quetiapine if Telithromycin is initiated, discontinued or dose changed.
Quinidine Co-administration may result in altered plasma concentrations of Quinidine and/or Telithromycin. Consider alternate therapy or monitor the therapeutic/adverse effects of both agents.
Quinidine Increased risk of cardiotoxicity and arrhythmias
Quinidine barbiturate Increased risk of cardiotoxicity and arrhythmias
Quinine Telithromycin may reduce clearance of Quinine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Quinine if Telithromycin is initiated, discontinued or dose changed.
Ranolazine Increased levels of ranolazine - risk of toxicity
Ranolazine Telithromycin may reduce clearance of Ranolazine. Concomitant therapy should be avoided.
Repaglinide Telithromycin may reduce clearance of Repaglinide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Repaglinide if Telithromycin is initiated, discontinued or dose changed.
Rifabutin Rifabutin may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Rifampin Rifampin decreases the effect of telithromycin
Rifampin Rifampin may decrease the plasma concentration of Telithromycin. Concomitant therapy should be avoided.
Rifapentine Rifapentine may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
Ritonavir Ritonavir may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Salmeterol Telithromycin may reduce clearance of Salmeterol. Concomitant therapy is contraindicated.
Saquinavir Saquinavir may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Sibutramine Telithromycin may reduce clearance of Sibutramine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Sibutramine if Telithromycin is initiated, discontinued or dose changed.
Sildenafil Telithromycin may reduce clearance of Sildenafil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Sildenafil if Telithromycin is initiated, discontinued or dose changed.
Simvastatin Telithromycin may possibly increase statin toxicity
Simvastatin Telithromycin may reduce clearance of Simvastatin. Concomitant therapy is contraindicated.
Sirolimus Telithromycin may reduce clearance of Sirolimus. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Sirolimus if Telithromycin is initiated, discontinued or dose changed.
Solifenacin Telithromycin may reduce clearance of Solifenacin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Solifenacin if Telithromycin is initiated, discontinued or dose changed.
Sotalol Increased risk of cardiotoxicity and arrhythmias
Sotalol Telithromycin may decrease the absorption and efficacy of Sotalol.
Spiramycin Telithromycin may reduce clearance of Spiramycin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Spiramycin if Telithromycin is initiated, discontinued or dose changed.
Sufentanil Telithromycin may reduce clearance of Sufentanil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Sufentanil if Telithromycin is initiated, discontinued or dose changed.
Sunitinib Possible increase in sunitinib levels
Sunitinib Telithromycin may reduce clearance of Sunitinib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Sunitinib if Telithromycin is initiated, discontinued or dose changed.
Tacrolimus Telithromycin may reduce clearance of Tacrolimus. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tacrolimus if Telithromycin is initiated, discontinued or dose changed.
Tacrolimus This antibiotic increases the effect and toxicity of tacrolimus
Tadalafil Telithromycin may reduce clearance of Tadalafil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tadalafil if Telithromycin is initiated, discontinued or dose changed.
Tamoxifen Telithromycin may reduce clearance of Tamoxifen. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tamoxifen if Telithromycin is initiated, discontinued or dose changed.
Tamsulosin Telithromycin may reduce clearance of Tamsulosin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tamsulosin if Telithromycin is initiated, discontinued or dose changed.
Temsirolimus Telithromycin may reduce clearance of Temsirolimus. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Temsirolimus if Telithromycin is initiated, discontinued or dose changed.
Temsirolimus This CYP3A4 inhibitor increases the level of temsirolimus
Teniposide Telithromycin may reduce clearance of Teniposide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Teniposide if Telithromycin is initiated, discontinued or dose changed.
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Tetrabenazine Telithromycin may increase the QTc-prolonging effect of Tetrabenazine. Concomitant therapy should be avoided.
Theophylline Telithromycin may reduce clearance of Theophylline. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Theophylline if Telithromycin is initiated, discontinued or dose changed.
Thioridazine Telithromycin may increase the QTc-prolonging effect of Thioridazine. Concomitant therapy should be avoided.
Tiagabine Telithromycin may reduce clearance of Tiagabine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Telithromycin is initiated, discontinued or dose changed.
Tolterodine Telithromycin may reduce clearance of Tolterodine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tolterodine if Telithromycin is initiated, discontinued or dose changed.
Tramadol Telithromycin may reduce clearance of Tramadol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tramadol if Telithromycin is initiated, discontinued or dose changed.
Trazodone Telithromycin may reduce clearance of Trazodone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Trazodone if Telithromycin is initiated, discontinued or dose changed.
Triazolam Telithromycin increases the effect/toxicity of the benzodiazepine
Triazolam Telithromycin may reduce clearance of Triazolam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Triazolam if Telithromycin is initiated, discontinued or dose changed.
Trimipramine Telithromycin may reduce clearance of Trimipramine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Trimipramine if Telithromycin is initiated, discontinued or dose changed.
Vardenafil Telithromycin may reduce clearance of Vardenafil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Vardenafil if Telithromycin is initiated, discontinued or dose changed.
Venlafaxine Telithromycin may reduce clearance of Venlafaxine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Venlafaxine if Telithromycin is initiated, discontinued or dose changed.
Verapamil Telithromycin may possibly increase verapamil effect/toxicity
Verapamil Telithromycin may reduce clearance of Verapamil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Verapamil if Telithromycin is initiated, discontinued or dose changed.
Vinblastine Telithromycin may reduce clearance of Vinblastine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Vinblastine if Telithromycin is initiated, discontinued or dose changed.
Vincristine Telithromycin may reduce clearance of Vincristine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Vincristine if Telithromycin is initiated, discontinued or dose changed.
Vinorelbine Telithromycin may reduce clearance of Vinorelbine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Vinorelbine if Telithromycin is initiated, discontinued or dose changed.
Voriconazole Voriconazole may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
Warfarin Telithromycin increases the anticoagulant effect
Warfarin Telithromycin may increase the anticoagulant effect of Warfarin. INR should be monitored and Warfarin dose adjusted accordingly during concomitant therapy.
Ziprasidone Telithromycin may increase the QTc-prolonging effect of Ziprasidone. Concomitant therapy should be avoided.
Zolpidem Telithromycin may reduce clearance of Zolpidem. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Zolpidem if Telithromycin is initiated, discontinued or dose changed.
Zonisamide Telithromycin may reduce clearance of Zonisamide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Zonisamide if Telithromycin is initiated, discontinued or dose changed.
Zopiclone Telithromycin may reduce clearance of Zopiclone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Zopiclone if Telithromycin is initiated, discontinued or dose changed.
ambrisentan Telithromycin may reduce clearance of Ambrisentan. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ambrisentan if Telithromycin is initiated, discontinued or dose changed.
armodafinil Telithromycin may reduce clearance of Armodafinil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Armodafinil if Telithromycin is initiated, discontinued or dose changed.
doxorubicin TransDrug Telithromycin may reduce clearance of Doxorubicin. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Doxorubicin if Telithromycin is initiated, discontinued or dose changed.
rivaroxaban Telithromycin may reduce clearance of Rivaroxaban. Concomitant therapy is contraindicated.
Food Interactions
  • Take without regard to meals.
Pathways Not Available
General References
  1. Clay KD, Hanson JS, Pope SD, Rissmiller RW, Purdum PP 3rd, Banks PM: Brief communication: severe hepatotoxicity of telithromycin: three case reports and literature review. Ann Intern Med. 2006 Mar 21;144(6):415-20. Epub 2006 Feb 15. [PubMed Link Image]
  2. Drugs.com Link Image
  3. Wikipedia Link Image
  4. RxList Link Image
  5. PDRhealth Link Image
Organisms Affected
  • Enteric bacteria and other eubacteria
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 3A4 (CYP3A4)
  2. Cytochrome P450 1A2 (CYP1A2)
Targets
  1. 23S rRNA
  2. Cytochrome P450 3A3
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 3A4 (CYP3A4)
Enzyme 1 Gene Name CYP3A4
Enzyme 1 SwissProt ID P08684 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P08684|CP3A4_HUMAN Cytochrome P450 3A4 (EC 1.14.13.67) 
ALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFD
MECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIA
EDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSM
DVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVF
PREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSII
FIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVN
ETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERFSK
KNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGG
LLQPEKPVVLKVESRDGTVSGA
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name Cytochrome P450 1A2 (CYP1A2)
Enzyme 2 Gene Name CYP1A2
Enzyme 2 SwissProt ID P05177 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >P05177|CP1A2_HUMAN Cytochrome P450 1A2 - Homo sapiens (Human). 
MALSQSVPFSATELLLASAIFCLVFWVLKGLRPRVPKGLKSPPEPWGWPLLGHVLTLGKN
PHLALSRMSQRYGDVLQIRIGSTPVLVLSRLDTIRQALVRQGDDFKGRPDLYTSTLITDG
QSLTFSTDSGPVWAARRRLAQNALNTFSIASDPASSSSCYLEEHVSKEAKALISRLQELM
AGPGHFDPYNQVVVSVANVIGAMCFGQHFPESSDEMLSLVKNTHEFVETASSGNPLDFFP
ILRYLPNPALQRFKAFNQRFLWFLQKTVQEHYQDFDKNSVRDITGALFKHSKKGPRASGN
LIPQEKIVNLVNDIFGAGFDTVTTAISWSLMYLVTKPEIQRKIQKELDTVIGRERRPRLS
DRPQLPYLEAFILETFRHSSFLPFTIPHSTTRDTTLNGFYIPKKCCVFVNQWQVNHDPEL
WEDPSEFRPERFLTADGTAINKPLSEKMMLFGMGKRRCIGEVLAKWEIFLFLAILLQQLE
FSVPPGVKVDLTPIYGLTMKHARCEHVQARRFSIN
Drug Target 1 [top]
Target 1 ID 884
Target 1 Name 23S rRNA
Target 1 Synonyms
  1. 23S ribosomal ribonucleic acid
Target 1 Gene Name Not Available
Target 1 Protein Sequence Not Available
Target 1 Number of Residues 0
Target 1 Molecular Weight Not Available
Target 1 Theoretical pI Not Available
Target 1 GO Classification
Function
transferase activity
translation
RNA binding
Process
rRNA processing
RNA processing and modification
Component
cell
Target 1 General Function Translation, ribosomal structure and biogenesis
Target 1 Specific Function In prokaryotes, the 23S rRNA is part of the large subunit (the 50S) that joins with the 30S small subunit to create the functional 70S ribosome. The ribosome is comprised of 3 RNAs: the 23S, the 16S and the 5S ribosomal RNAs. The 23S and the 5S associate with their respective proteins to make up the large subunit of the ribosome, while the 16S RNA associates with its proteins to make up the small subunit.
Target 1 Pathways
Name SMPDB Link KEGG Link
Ribosome map03010 Link Image
Target 1 Reactions
  • tRNA-aminoacid + ATP + polypeptide(n) = polypeptide(n+1) + ADP
Target 1 Pfam Domain Function Not Available
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • None
Target 1 Essentiality Essential
Target 1 GenBank ID Protein Not Available
Target 1 UniProtKB/Swiss-Prot ID Not Available
Target 1 UniProtKB/Swiss-Prot Entry Name Not Available
Target 1 PDB ID 1EMI Link Image
Target 1 PDB File Show
Target 1 3D Structure
Target 1 Cellular Location
  • Cytoplasmic
Target 1 Gene Sequence >23S rRNA sequence 
GATTAAGTTATTAAGGGCGCACGGTGGATGCCTTGGCACTAGAAGCCGATGAAGGACGTT
ACTAACGACGATATGCTTTGGGGAGCTGTAAGTAAGCTTTGATCCAGAGATTTCCGAATG
GGGAAACCCAGCATGAGTTATGTCATGTTATCGATATGTGAATACATAGCATATCAGAAG
GCACACCCGGAGAACTGAAACATCTTAGTACCCGGAGGAAGAGAAAGAAAATTCGATTCC
CTTAGTAGCGGCGAGCGAAATGGGAAGAGCCCAAACCAACAAGCTTGCTTGTTGGGGTTG
TAGGACACTCTATACGGAGTTACAAAGGACGACATTAGACGAATCATCTGGAAAGATGAA
TCAAAGAAGGTAATAATCCTGTAGTCGAAAATGTTGTCTCTCTTGAGTGGATCCTGAGTA
CGACGGAGCACGTGAAATTCCGTCGGAATCTGGGAGGACCATCTCCTAAGGCTAAATACT
CTCTAGTGACCGATAGTGAACCAGTACCGTGAGGGAAAGGTGAAAAGCACCCCGGAAGGG
GAGTGAAATAGAACCTGAAACCGTGTGCTTACAAGTAGTCAGAGCCCGTTAATGGGTGAT
GGCGTGCCTTTTGTAGAATGAACCGGCGAGTTACGATTTGATGCAAGGTTAAGCAGTAAA
TGTGGAGCCGTAGCGAAAGCGAGTCTGAATAGGGCGTTTAGTATTTGGTCGTAGACCCGA
AACCAGGTGATCTACCCTTGGTCAGGTTGAAGTTCAGGTAACACTGAATGGAGGACCGAA
CCGACTTACGTTGAAAAGTGAGCGGATGAACTGAGGGTAGCGGAGAAATTCCAATCGAAC
CTGGAGATAGCTGGTTCTCTCCGAAATAGCTTTAGGGCTAGCCTCAAGTGATGATTATTG
GAGGTAGAGCACTGTTTGGACGAGGGGCCCCTCTCGGGTTACCGAATTCAGACAAACTCC
GAATGCCAATTAATTTAACTTGGGAGTCAGAACATGGGTGATAAGGTCCGTGTTCGAAAG
GGAAACAGCCCAGACCACCAGCTAAGGTCCCAAAATATATGTTAAGTGGAAAAGGATGTG
GCGTTGCCCAGACAACTAGGATGTTGGCTTAGAAGCAGCCATCATTTAAAGAGTGCGTAA
TAGCTCACTAGTCGAGTGACACTGCGCCGAAAATGTACCGGGGCTAAACATATTACCGAA
GCTGTGGATTGTCCTTTGGACAATGGTAGGAGAGCGTTCTAAGGGCGTTGAAGCATGATC
GTAAGGACATGTGGAGCGCTTAGAAGTGAGAATGCCGGTGTGAGTAGCGAAAGACGGGTG
AGAATCCCGTCCACCGATTGACTAAGGTTTCCAGAGGAAGGCTCGTCCGCTCTGGGTTAG
TCGGGTCCTAAGCTGAGGCCGACAGGCGTAGGCGATGGATAACAGGTTGATATTCCTGTA
CCACCTATAATCGTTTTAATCGATGGGGGGACGCAGTAGGATAGGCGAAGCGTGCGATTG
GATTGCACGTCTAAGCAGTAAGGCTGAGTATTAGGCAAATCCGGTACTCGTTAAGGCTGA
GCTGTGATGGGGAGAAGACATTGTGTCTTCGAGTCGTTGATTTCACACTGCCGAGAAAAG
CCTCTAGATAGAAAATAGGTGCCCGTACCGCAAACCGACACAGGTAGTCAAGATGAGAAT
TCTAAGGTGAGCGAGCGAACTCTCGTTAAGGAACTCGGCAAAATGACCCCGTAACTTCGG
GAGAAGGGGTGCTCTTTAGGGTTAACGCCCAGAAGAGCCGCAGTGAATAGGCCCAAGCGA
CTGTTTATCAAAAACACAGGTCTCTGCTAAACCGTAAGGTGATGTATAGGGGCTGACGCC
TGCCCGGTGCTGGAAGGTTAAGAGGAGTGGTTAGCTTCTGCGAAGCTACGAATCGAAGCC
CCAGTAAACGGCGGCCGTAACTATAACGGTCCTAAGGTAGCGAAATTCCTTGTCGGGTAA
GTTCCGACCCGCACGAAAGGCGTAACGATTTGGGCACTGTCTCAACGAGAGACTCGGTGA
AATCATAGTACCTGTGAAGATGCAGGTTACCCGCGACAGGACGGAAAGACCCCGTGGAGC
TTTACTGTAGCCTGATATTGAAATTCGGCACAGCTTGTACAGGATAGGTAGGAGCCTTTG
AAACGTGAGCGCTAGCTTACGTGGAGGCGCTGGTGGGATACTACCCTAGCTGTGTTGGCT
TTCTAACCCGCACCACTTATCGTGGTGGGAGACAGTGTCAGGCGGGCAGTTTGACTGGGG
CGGTCGCCTCCTAAAAGGTAACGGAGGCGCTCAAAGGTTCCCTCAGAATGGTTGGAAATC
ATTCATAGAGTGTAAAGGCATAAGGGAGCTTGACTGCGAGACCTACAAGTCGAGCAGGGT
CGAAAGACGGACTTAGTGATCCGGTGGTTCCGCATGGAAGGGCCATCGCTCAACGGATAA
AAGCTACCCCGGGGATAACAGGCTTATCTCCCCCAAGAGTTCACATCGACGGGGAGGTTT
GGCACCTCGATGTCGGCTCATCGCATCCTGGGGCTGTAGTCGGTCCCAAGGGTTGGGCTG
TTCGCCCATTAAAGCGGTACGCGAGCTGGGTTCAGAACGTCGTGAGACAGTTCGGTCCCT
ATCCGTCGTGGGCGTAGGAAATTTGAGAGGAGCTGTCCTTAGTACGAGAGGACCGGGATG
GACATACCTCTGGTGTACCAGTTGTCGTGCCAACGGCATAGCTGGGTAGCTATGTGTGGA
CGGGATAAGTGCTGAAAGCATCTAAGCATGAAGCCCCCCTCAAGATGAGATTTCCCAACT
TCGGTTATAAGATCCCTCAAAGATGATGAGGTTAATAGGTTCGAGGTGGAAGCATGGTGA
CATGTGGAGCTGACGAATACTAATCGATCGAAGACTTAATCAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID Not Available
Target 1 GenAtlas ID Not Available
Target 1 HGNC ID Not Available
Target 1 Chromosome Location Not Available
Target 1 Locus Not Available
Target 1 SNPs Not Available
Target 1 General References
  1. Barrett JF: Linezolid Pharmacia Corp. Curr Opin Investig Drugs. 2000 Oct;1(2):181-7. [PubMed Link Image]
Target 1 Drug References
  1. Reinert RR, Al-Lahham A: Time-kill study of the activity of telithromycin against macrolide-resistant Streptococcus pneumoniae Isolates with 23S rRNA mutations and changes in ribosomal proteins L4 and L22. Antimicrob Agents Chemother. 2005 Jul;49(7):3011-3. [PubMed Link Image]
  2. Farrell DJ, Shackcloth J, Barbadora KA, Green MD: Streptococcus pyogenes isolates with high-level macrolide resistance and reduced susceptibility to telithromycin associated with 23S rRNA mutations. Antimicrob Agents Chemother. 2006 Feb;50(2):817-8. [PubMed Link Image]
  3. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  4. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
  5. Hirakata Y, Mizuta Y, Wada A, Kondoh A, Kurihara S, Izumikawa K, Seki M, Yanagihara K, Miyazaki Y, Tomono K, Kohno S: The first telithromycin-resistant Streptococcus pneumoniae isolate in Japan associated with erm(B) and mutations in 23S rRNA and riboprotein L4. Jpn J Infect Dis. 2007 Feb;60(1):48-50. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 1337
Target 2 Name Cytochrome P450 3A3
Target 2 Synonyms
  1. CYPIIIA3
  2. EC 1.14.14.1
  3. HLp
Target 2 Gene Name CYP3A3
Target 2 Protein Sequence >Cytochrome P450 3A3 
MALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMF
DMECHKKYGKVWGFYDGQQPVLAITDPDMIKLVLVKECYSVFTNREPFGPVGFMKSAISI
AEDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRRERETGKPVTLKDVFGAYS
MDVITSSSFGVNVDSLNNPQDPLVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICV
FPREVTNFLRKAVKRMKESRLEDTQKHRVDFLQLMIDSHKNSKETESHKALSDLELVAQS
IIFIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMV
VNETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERF
SKKNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSL
GGLLQPEKPVVLKVESRDGTVSGA
Target 2 Number of Residues 512
Target 2 Molecular Weight 57560
Target 2 Theoretical pI 8.25
Target 2 GO Classification
Function
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
tetrapyrrole binding
heme binding
binding
ion binding
cation binding
transition metal ion binding
iron ion binding
catalytic activity
oxidoreductase activity
monooxygenase activity
Process
physiological process
metabolism
cellular metabolism
generation of precursor metabolites and energy
electron transport
Component
Not Available
Target 2 General Function Secondary metabolites biosynthesis, transport and catabolism
Target 2 Specific Function Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics
Target 2 Pathways
Name SMPDB Link KEGG Link
Fatty acid metabolism SMP00051 Link Image map00071 Link Image
Target 2 Reactions
  • RH + reduced flavoprotein + O2 = ROH + oxidized flavoprotein + H2O
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • None
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 219963 Link Image
Target 2 UniProtKB/Swiss-Prot ID P05184 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name CP3A3_HUMAN Link Image
Target 2 PDB ID 1TQN Link Image
Target 2 PDB File Show
Target 2 3D Structure
Target 2 Cellular Location
  • Endoplasmic reticulum
  • endoplasmic reticulum membrane
  • peripheral membrane protein
Target 2 Gene Sequence >1515 bp 
ATGGCTCTCATCCCAGACTTGGCCATGGAAACCTGGCTTCTCCTGGCTGTCAGCCTGGTG
CTCCTCTATCTATATGGAACCCATTCACATGGACTTTTTAAGAAGCTTGGAATTCCAGGG
CCCACACCTCTGCCTTTTTTGGGAAATATTTTGTCCTACCATAAGGGCTTTTGTATGTTT
GACATGGAATGTCATAAAAAGTATGGAAAAGTGTGGGGCTTTTATGATGGTCAACAGCCT
GTGCTGGCTATCACAGATCCTGACATGATCAAACTAGTGCTAGTGAAAGAATGTTATTCT
GTCTTCACAAACCGCGAGCCTTTTGGTCCAGTGGGATTTATGAAAAGTGCCATCTCTATA
GCTGAGGATGAAGAATGGAAGAGATTACGATCATTGCTGTCTCCAACCTTCACCAGTGGA
AAACTCAAGGAGATGGTCCCTATCATTGCCCAGTATGGAGATGTGTTGGTGAGAAATCTG
AGGCGGGAACGAGAGACAGGCAAGCCTGTCACCTTGAAAGACGTCTTTGGGGCCTACAGC
ATGGATGTGATCACTAGCTCATCATTTGGAGTGAACGTCGACTCTCTCAACAATCCACAG
GACCCCCTTGTGGAAAACACCAAGAAGCTTTTAAGATTTGATTTTTTGGATCCATTCTTT
CTCTCAATAACAGTCTTTCCATTCCTCATCCCAATTCTTGAAGTATTAAATATCTGTGTG
TTTCCAAGAGAAGTTACAAATTTTTTAAGAAAAGCTGTAAAAAGGATGAAAGAAAGTCGC
CTCGAAGATACACAAAAGCACCGAGTGGATTTCCTTCAGCTGATGATTGACTCTCATAAG
AATTCAAAAGAAACTGAGTCCCACAAAGCTCTGTCCGATCTGGAGCTCGTGGCCCAATCA
ATTATCTTTATTTTTGCTGGCTATGAAACCACGAGCAGTGTTCTCTCCTTCATTATGTAT
GAACTGGCCACTCACCCTGATGTCCAGCAGAAACTGCAGGAGGAAATTGATGCAGTTTTA
CCCAATAAGGCACCACCCACCTATGATACTGTGCTACAGATGGAGTATCTTGACATGGTG
GTGAATGAAACGCTCAGATTATTCCCAATTGCTATGAGACTTGAGAGGGTCTGCAAAAAA
GATGTTGAGATCAATGGGATGTTCATTCCCAAAGGGTGGGTGGTGATGATTCCAAGCTAT
GCTCTTCACCGTGACCCAAAGTACTGGACAGAGCCTGAGAAGTTCCTCCCTGAAAGATTC
AGCAAGAAGAACAAGGACAACATAGATCCTTACATATACACACCCTTTGGAAGTGGACCC
AGAAACTGCATTGGCATGAGGTTTGCTCTCATGAACATGAAACTTGCTCTAATCAGAGTC
CTTCAGAACTTCTCCTTCAAACCTTGTAAAGAAACACAGATCCCCCTGAAATTAAGCTTA
GGAGGACTTCTTCAACCAGAAAAACCCGTTGTTCTAAAGGTTGAGTCAAGGGATGGCACC
GTAAGTGGAGCCTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID CYP3A3 Link Image
Target 2 GenAtlas ID CYP3A3 Link Image
Target 2 HGNC ID HGNC:2636 Link Image
Target 2 Chromosome Location 7
Target 2 Locus 7q21.1
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Molowa DT, Schuetz EG, Wrighton SA, Watkins PB, Kremers P, Mendez-Picon G, Parker GA, Guzelian PS: Complete cDNA sequence of a cytochrome P-450 inducible by glucocorticoids in human liver. Proc Natl Acad Sci U S A. 1986 Jul;83(14):5311-5. [PubMed Link Image]
  2. Watkins PB, Wrighton SA, Maurel P, Schuetz EG, Mendez-Picon G, Parker GA, Guzelian PS: Identification of an inducible form of cytochrome P-450 in human liver. Proc Natl Acad Sci U S A. 1985 Sep;82(18):6310-4. [PubMed Link Image]
Target 2 Drug References
  1. Bearden DT, Neuhauser MM, Garey KW: Telithromycin: an oral ketolide for respiratory infections. Pharmacotherapy. 2001 Oct;21(10):1204-22. [PubMed Link Image]
  2. Zhanel GG, Walters M, Noreddin A, Vercaigne LM, Wierzbowski A, Embil JM, Gin AS, Douthwaite S, Hoban DJ: The ketolides: a critical review. Drugs. 2002;62(12):1771-804. [PubMed Link Image]
  3. Reed M, Wall GC, Shah NP, Heun JM, Hicklin GA: Verapamil toxicity resulting from a probable interaction with telithromycin. Ann Pharmacother. 2005 Feb;39(2):357-60. Epub 2004 Dec 14. [PubMed Link Image]
  4. Shi J, Chapel S, Montay G, Hardy P, Barrett JS, Sica D, Swan SK, Noveck R, Leroy B, Bhargava VO: Effect of ketoconazole on the pharmacokinetics and safety of telithromycin and clarithromycin in older subjects with renal impairment. Int J Clin Pharmacol Ther. 2005 Mar;43(3):123-33. [PubMed Link Image]
  5. Nguyen M, Chung EP: Telithromycin: the first ketolide antimicrobial. Clin Ther. 2005 Aug;27(8):1144-63. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.