troleandomycin

Summary

Summary: A macrolide antibiotic that is similar to ERYTHROMYCIN.

Top Publications

  1. Ball B, Hill M, Brenner M, Sanks R, Szefler S. Effect of low-dose troleandomycin on glucocorticoid pharmacokinetics and airway hyperresponsiveness in severely asthmatic children. Ann Allergy. 1990;65:37-45 pubmed
    ..randomized, parallel, double-blind placebo-controlled comparison of combination methylprednisolone and placebo troleandomycin, prednisone and troleandomycin (P-TAO) or methylprednisolone-TAO (MPn-TAO)...
  2. Garzotti M, Rovatti L, Hamdan M. Coupling of a supercritical fluid chromatography system to a hybrid (Q-TOF 2) mass spectrometer: on-line accurate mass measurements. Rapid Commun Mass Spectrom. 2001;15:1187-90 pubmed
  3. Fowler S, Taylor J, Friedberg T, Wolf C, Riley R. CYP3A4 active site volume modification by mutagenesis of leucine 211. Drug Metab Dispos. 2002;30:452-6 pubmed
    ..Furthermore, IC50 values for the inhibition of testosterone 6 beta-hydroxylation by erythromycin and troleandomycin for L211F were 2.4- and 3.7-fold higher, and those for L211Y were 3.4- and 9...
  4. Franklin M, Phillips J, Kushner J. CYP3A-inducing agents and the attenuation of uroporphyrin accumulation and excretion in a rat model of porphyria cutanea tarda. Biochem Pharmacol. 2000;60:1325-31 pubmed
    ..Attenuation of porphyrin accumulation could also be demonstrated with daily troleandomycin treatment...
  5. He N, Huang S, Zhu R, Tan Z, Liu J, Zhu B, et al. Inhibitory effect of troleandomycin on the metabolism of omeprazole is CYP2C19 genotype-dependent. Xenobiotica. 2003;33:211-21 pubmed
    ..CYP2C19 genotyped male subjects were administered a 20-mg oral dose of omeprazole (OP) alone or received troleandomycin (TAO) 500 mg daily for 2 days before the dose of OP was administered...
  6. Xu Y, Hashizume T, Shuhart M, Davis C, Nelson W, Sakaki T, et al. Intestinal and hepatic CYP3A4 catalyze hydroxylation of 1alpha,25-dihydroxyvitamin D(3): implications for drug-induced osteomalacia. Mol Pharmacol. 2006;69:56-65 pubmed
    ..These and other data suggest that induction of CYP3A4-dependent 1,25(OH)(2)D(3) metabolism by antiepileptic drugs and other PXR ligands may diminish intestinal effects of the hormone and contribute to osteomalacia. ..
  7. Trubetskoy O, Marks B, Zielinski T, Yueh M, Raucy J. A simultaneous assessment of CYP3A4 metabolism and induction in the DPX-2 cell line. AAPS J. 2005;7:E6-13 pubmed
  8. Vaclavikova R, Soucek P, Svobodova L, Anzenbacher P, Simek P, Guengerich F, et al. Different in vitro metabolism of paclitaxel and docetaxel in humans, rats, pigs, and minipigs. Drug Metab Dispos. 2004;32:666-74 pubmed
    ..b>Troleandomycin as a selective inhibitor of CYP3A inhibited the formation of C3'-OHP, C2-OHP, and di-OHP, as well as the ..
  9. Ufer M, Svensson J, Krausz K, Gelboin H, Rane A, Tybring G. Identification of cytochromes P450 2C9 and 3A4 as the major catalysts of phenprocoumon hydroxylation in vitro. Eur J Clin Pharmacol. 2004;60:173-82 pubmed
    ..Increased vigilance is warranted when PPC treatment is combined with substrates, inhibitors, or inducers of these enzymes. ..

More Information

Publications62

  1. Yoshimoto K, Echizen H, Chiba K, Tani M, Ishizaki T. Identification of human CYP isoforms involved in the metabolism of propranolol enantiomers--N-desisopropylation is mediated mainly by CYP1A2. Br J Clin Pharmacol. 1995;39:421-31 pubmed
    ..In contrast, sulphaphenazole (CYP2C8/9 inhibitor), S-mephenytoin (CYP2C19 inhibitor), troleandomycin (CYP3A3/4 inhibitor) and diethyldithiocarbamate (CYP2E1 inhibitor) elicited only weak inhibitory effects on ..
  2. Honda A, Salen G, Matsuzaki Y, Batta A, Xu G, Leitersdorf E, et al. Side chain hydroxylations in bile acid biosynthesis catalyzed by CYP3A are markedly up-regulated in Cyp27-/- mice but not in cerebrotendinous xanthomatosis. J Biol Chem. 2001;276:34579-85 pubmed
    ..b>Troleandomycin, a specific inhibitor of CYP3A, markedly suppressed these microsomal side chain hydroxylations in both mouse ..
  3. Witkamp R, Nijmeijer S, Van Miert A. Cytochrome P-450 complex formation in rat liver by the antibiotic tiamulin. Antimicrob Agents Chemother. 1996;40:50-4 pubmed
    ..It is concluded that tiamulin is a potent and selective inducer-inhibitor of cytochrome P-450. Though not belonging to the macrolides, the compound produces an effect on P-450 similar to those of TAO and related compounds. ..
  4. Brain E, Yu L, Gustafsson K, Drewes P, Waxman D. Modulation of P450-dependent ifosfamide pharmacokinetics: a better understanding of drug activation in vivo. Br J Cancer. 1998;77:1768-76 pubmed
    ..05), whereas the P450 inhibitors orphenadrine and troleandomycin had no significant affect on AUC values...
  5. Yamamoto T, Suzuki A, Kohno Y. High-throughput screening for the assessment of time-dependent inhibitions of new drug candidates on recombinant CYP2D6 and CYP3A4 using a single concentration method. Xenobiotica. 2004;34:87-101 pubmed
    ..the test compounds studied, ketoconazole inhibited CYP3A4 activity most extensively, followed by miconazole, troleandomycin, terfenazine and midazolam...
  6. Shimada H, Furuno H, Hirai K, Koyama J, Ariyama J, Simamura E. Paraquat detoxicative system in the mouse liver postmitochondrial fraction. Arch Biochem Biophys. 2002;402:149-57 pubmed
    ..pretreated with CoCl(2) (a CYP synthesis inhibitor) or SKF 525-A (a CYP inhibitor) were dead after 5 days, and troleandomycin (a CYP3A-specific inhibitor) also reduced the survival rate...
  7. Shang J, Xu S, Teffera Y, Doss G, Stearns R, Edmonson S, et al. Metabolic activation of a pentafluorophenylethylamine derivative: formation of glutathione conjugates in vitro in the rat. Xenobiotica. 2005;35:697-713 pubmed
    ..In incubations with pooled rat liver microsomes and recombinant rat CYP3A1 and CYP3A2, troleandomycin (TAO) reduced the formation of GSH conjugates M2-4 by 80-90%, but it had no effect on the formation of M1...
  8. Chen Q, Doss G, Tung E, Liu W, Tang Y, Braun M, et al. Evidence for the bioactivation of zomepirac and tolmetin by an oxidative pathway: identification of glutathione adducts in vitro in human liver microsomes and in vivo in rats. Drug Metab Dispos. 2006;34:145-51 pubmed
  9. Wolf K, Wood S, Allard J, Hunt J, Gorman N, Walton Strong B, et al. Role of CYP3A and CYP2E1 in alcohol-mediated increases in acetaminophen hepatotoxicity: comparison of wild-type and Cyp2e1(-/-) mice. Drug Metab Dispos. 2007;35:1223-31 pubmed
    ..In conclusion, these findings suggest that both CYP3A and CYP2E1 contribute to APAP hepatotoxicity in alcohol-treated mice. ..
  10. G├╝rel G, Blaha G, Steitz T, Moore P. Structures of triacetyloleandomycin and mycalamide A bind to the large ribosomal subunit of Haloarcula marismortui. Antimicrob Agents Chemother. 2009;53:5010-4 pubmed publisher
    ..Mycalamide A binds to the E site and inhibits protein synthesis by occupying the space normally occupied by the CCA end of E-site-bound tRNAs...
  11. Grimsley A, Gallagher R, Hutchison M, Pickup K, Wilson I, Samuelsson K. Drug-drug interactions and metabolism in cytochrome P450 2C knockout mice: application to troleandomycin and midazolam. Biochem Pharmacol. 2013;86:529-38 pubmed publisher
    ..KO) mouse was investigated for studying DDIs using midazolam (MDZ) a standard human CYP3A4 substrate and troleandomycin (TAO) a potent human CYP3A4 inhibitor...
  12. Liu X, Ren Y, Qian Z, Wang G. Enzyme kinetics and inhibition of nimodipine metabolism in human liver microsomes. Acta Pharmacol Sin. 2000;21:690-4 pubmed
    ..The dehydrogenation of dihydropyridine ring of NDP was competitively inhibited by ketoconazole (Ket) and troleandomycin (TAO), and the Ki values for Ket and TAO were 0.59 and 122.2 mumol, respectively...
  13. Menz G, Rothe T, Schmitt M, Schmitz M, Hauser F, Haack D, et al. [Experiences with a combination therapy of methylprednisolone and troleandomycin in severe bronchial asthma requiring high-dose corticoids]. Pneumologie. 1990;44 Suppl 1:238-40 pubmed
    Although treatment comprising a combination of methylprednisolone (MP) and troleandomycin (TAO) has been employed to treat cases of severe bronchial asthma requiring high doses of corticosteroids, for about 20 years, now, it has always ..
  14. Tuvesson H, Wienkers L, Gunnarsson P, Seidegard J, Persson R. Identification of cytochrome P4503A as the major subfamily responsible for the metabolism of roquinimex in man. Xenobiotica. 2000;30:905-14 pubmed
    ..significant inhibition (>90%) of roquinimex primary metabolism was demonstrated by ketoconazole and troleandomycin, specific inhibitors of CYP3A4 as well as with anti-CYP3A4 antibodies...
  15. Spector S. Alternative treatments in the patient with intractable asthma. Curr Opin Pulm Med. 1997;3:23-9 pubmed
    ..The antileukotrienes represent a safe class of medications that may be of particular benefit to certain subgroups of asthmatic patients. Antileukotrienes have become commercially available in other countries. ..
  16. Zhang Y, Quan Y. [Involvement of cytochrome P4503A in the monohydroxylation of ring A of praziquantel in rat liver microsomes]. Yao Xue Xue Bao. 1997;32:5-10 pubmed
    ..The rates of ring A monohydroxylate formation were strongly correlated with the activity of N-demethylase of ERY and EMP. These results indicate that CYP3A is involved in the monohydroxylation of the ring A of PZQ. ..
  17. Choi Y, Lee M. Pharmacokinetic and pharmacodynamic interaction between nifedipine and metformin in rats: competitive inhibition for metabolism of nifedipine and metformin by each other via CYP isozymes. Xenobiotica. 2012;42:483-95 pubmed publisher
  18. Zhang L, Hu X, Wang P, Zhang L. [Metabolism of osthol in isolated hepatocytes of rat]. Yao Xue Xue Bao. 2009;44:1131-5 pubmed
    ..quercetin (Que), CYP2C9 inhibitor sulfaphenazole (Sul), CYP2D6 inhibitor yohimbine (Yoh), CYP3A4 inhibitor troleandomycin (Tro) and CYP450 inducer rifampicin (Rif) were used to investigate their effects on the metabolism of Ost...
  19. Kharasch E, Whittington D, Hoffer C, Krudys K, Craig K, Vicini P, et al. Paradoxical role of cytochrome P450 3A in the bioactivation and clinical effects of levo-alpha-acetylmethadol: importance of clinical investigations to validate in vitro drug metabolism studies. Clin Pharmacokinet. 2005;44:731-51 pubmed
    ..Subjects received oral LAAM (0.25 mg/kg) after CYP3A induction (rifampicin [rifampin]), inhibition (troleandomycin) or nothing (controls)...
  20. Klees T, Sheffels P, Dale O, Kharasch E. Metabolism of alfentanil by cytochrome p4503a (cyp3a) enzymes. Drug Metab Dispos. 2005;33:303-11 pubmed
    ..Effects of the CYP3A inhibitors troleandomycin and ketoconazole were also determined...
  21. Chepkwony H, Roets E, Hoogmartens J. Liquid chromatography of troleandomycin. J Chromatogr A. 2001;914:53-8 pubmed
    Until now no liquid chromatography (LC) method is described to determine the purity and content of troleandomycin and its related substances...
  22. Martinkova M, Kubickova B, Stiborova M. Effects of cytochrome P450 inhibitors on peroxidase activity. Neuro Endocrinol Lett. 2012;33 Suppl 3:33-40 pubmed
  23. Shu Y, Wang L, Xu Z, He N, Xiao W, Wang W, et al. 5-hydroxylation of omeprazole by human liver microsomal fractions from Chinese populations related to CYP2C19 gene dose and individual ethnicity. J Pharmacol Exp Ther. 2000;295:844-51 pubmed
    ..in vivo, the monoclonal antibody to CYP2C8/9/19 strongly inhibited 5-OH-OP formation in EM microsomes, whereas troleandomycin (TAO) eliminated most of the formation at a high substrate concentration...
  24. Baldwin A, Huang Z, Jounaidi Y, Waxman D. Identification of novel enzyme-prodrug combinations for use in cytochrome P450-based gene therapy for cancer. Arch Biochem Biophys. 2003;409:197-206 pubmed
    ..studies using liver microsomes from uninduced male and female rats and by using the CYP3A-selective inhibitors troleandomycin and ketoconazole...
  25. Honda A, Miyazaki T, Ikegami T, Iwamoto J, Maeda T, Hirayama T, et al. Cholesterol 25-hydroxylation activity of CYP3A. J Lipid Res. 2011;52:1509-16 pubmed publisher
    ..Furthermore, treatment of the cells with troleandomycin, a specific inhibitor of CYP3A, significantly reduced cellular 25-hydroxycholesterol concentrations...
  26. Liu Y, Zeng B, Shang H, Cen Y, Wei H. Bama miniature pigs (Sus scrofa domestica) as a model for drug evaluation for humans: comparison of in vitro metabolism and in vivo pharmacokinetics of lovastatin. Comp Med. 2008;58:580-7 pubmed
    ..From these results, we conclude that Bama miniature pigs are suitable for use in drug evaluation studies. ..
  27. Gupta R, He Y, Patrick K, Halpert J, Bell N. CYP3A4 is a vitamin D-24- and 25-hydroxylase: analysis of structure function by site-directed mutagenesis. J Clin Endocrinol Metab. 2005;90:1210-9 pubmed
    ..in recombinant CYP3A4 and pooled human liver microsomes showed dose-dependent inhibition by ketoconazole, troleandomycin, alpha-naphthoflavone, and isoniazid, known inhibitors of CYP3A4...
  28. Basu A, Hagley R, Ghosh S, Kramer L, Nance W, Watlington C. Maternal environment defines blood pressure and its response to troleandomycin in spontaneously hypertensive rats. Am J Hypertens. 1995;8:321-4 pubmed
    Relationship between family-3A cytochrome P-450-dependent (troleandomycin inhibitable) and maternal environmental-dependent systolic blood pressure (SBP) was investigated in spontaneously hypertensive rats (SHR)...
  29. Yang Z, Zhou S, Mei Q, Yang T, Liu Z. [Metabolic kinetics of MN9202 in Beagle dog liver microsomes]. Yao Xue Xue Bao. 2005;40:1019-23 pubmed
    ..The metabolism of MN9202 was significantly inhibited by ketoconazole (Ket) and troleandomycin (Tro) in Beagle dog liver microsomes. Tranylcypromine (Tra) could inhibit the metabolism of drug as well...
  30. Kharasch E, Hankins D, Fenstamaker K, Cox K. Human halothane metabolism, lipid peroxidation, and cytochromes P(450)2A6 and P(450)3A4. Eur J Clin Pharmacol. 2000;55:853-9 pubmed
    ..Patients (n = 9 each group) received single doses of the mechanism-based inhibitors troleandomycin (CYP3A4), methoxsalen (CYP2A6) or nothing (controls) before a standard halothane anaesthetic...
  31. Tateishi T, Watanabe M, Kumai T, Tanaka M, Moriya H, Yamaguchi S, et al. CYP3A is responsible for N-dealkylation of haloperidol and bromperidol and oxidation of their reduced forms by human liver microsomes. Life Sci. 2000;67:2913-20 pubmed
    ..In chemical and immunoinhibition studies, only troleandomycin and anti-CYP3A4 serum inhibited both formation rates of 4-fluorobenzoylpropionic acid, a metabolite of ..
  32. Perloff M, von Moltke L, Greenblatt D. Differential metabolism of midazolam in mouse liver and intestine microsomes: a comparison of cytochrome P450 activity and expression. Xenobiotica. 2003;33:365-77 pubmed
    ..5. MDZ hydroxylation is predominately CYP3A dependent in mouse intestine (compared with mouse liver) since CYP2C is not expressed in the intestine. The importance of CYP3A in the mouse intestine appears to mirror that in humans. ..
  33. Fujimaki Y, Arai N, Inaba T. Identification of cytochromes P450 involved in human liver microsomal metabolism of ecabapide, a prokinetic agent. Xenobiotica. 1999;29:1273-82 pubmed
    ..The formation of both metabolites was markedly decreased by ketoconazole, miconazole or troleandomycin (TAO), CYP3A-selective inhibitors, and also was inhibited by anti-CYP3A antibodies. 4...
  34. Kharasch E, Whittington D, Hoffer C. Influence of hepatic and intestinal cytochrome P4503A activity on the acute disposition and effects of oral transmucosal fentanyl citrate. Anesthesiology. 2004;101:729-37 pubmed
    ..10 microg/kg) after hepatic/intestinal CYP3A induction by rifampin, hepatic/intestinal CYP3A inhibition by troleandomycin, selective intestinal CYP3A inhibition by grapefruit juice, or nothing (control)...
  35. Shimada T, Guengerich F. Evidence for cytochrome P-450NF, the nifedipine oxidase, being the principal enzyme involved in the bioactivation of aflatoxins in human liver. Proc Natl Acad Sci U S A. 1989;86:462-5 pubmed
    ..in different liver samples, stimulation of activity by 7,8-benzoflavone, and inhibition of activity by troleandomycin. Similar results were obtained when levels of 2,3-dihydro-2-(N7-guanyl)-3-hydroxyaflatoxin B1 formed in DNA ..
  36. Sheffels P, Schroeder J, Altuntas T, Liggitt H, Kharasch E. Role of cytochrome P4503A in cysteine S-conjugates sulfoxidation and the nephrotoxicity of the sevoflurane degradation product fluoromethyl-2,2-difluoro-1-(trifluoromethyl)vinyl ether (compound A) in rats. Chem Res Toxicol. 2004;17:1177-89 pubmed
    ..Rats were pretreated with dexamethasone, phenobarbital, troleandomycin, or nothing (controls) before FDVE, and then, nephrotoxicity, FDVE-mercapturate sulfoxide urinary excretion, ..
  37. Ibrahim A, Feldman J, Karim A, Kharasch E. Simultaneous assessment of drug interactions with low- and high-extraction opioids: application to parecoxib effects on the pharmacokinetics and pharmacodynamics of fentanyl and alfentanil. Anesthesiology. 2003;98:853-61 pubmed
    ..and pharmacodynamics of the CYP3A substrates fentanyl and alfentanil compared with the CYP3A inhibitor troleandomycin. Alfentanil is a low-extraction drug with a clearance that is highly susceptible to drug interactions; ..
  38. Chen H, Fantel A, Juchau M. Catalysis of the 4-hydroxylation of retinoic acids by cyp3a7 in human fetal hepatic tissues. Drug Metab Dispos. 2000;28:1051-7 pubmed
    ..By contrast, troleandomycin strongly inhibited the reaction (70-75% inhibition), suggesting that CYP3A7 was primarily responsible for the ..
  39. Zhao X, Kawashiro T, Ishizaki T. Mutual inhibition between quinine and etoposide by human liver microsomes. Evidence for cytochrome P4503A4 involvement in their major metabolic pathways. Drug Metab Dispos. 1998;26:188-91 pubmed
    ..Two inhibitors of CYP3A4, ketoconazole (1 microM) and troleandomycin (100 microM), inhibited quinine 3-hydroxylation by about 90% and 80%, and etoposide 3'-demethylation by about ..
  40. Amunom I, Dieter L, Tamasi V, Cai J, CONKLIN D, Srivastava S, et al. Cytochromes P450 catalyze the reduction of ?,?-unsaturated aldehydes. Chem Res Toxicol. 2011;24:1223-30 pubmed publisher
    ..b>Troleandomycin increased HNA production 1...
  41. Meneses Lorente G, de Longueville F, Dos Santos Mendes S, Bonnert T, Jack A, Evrard S, et al. An evaluation of a low-density DNA microarray using cytochrome P450 inducers. Chem Res Toxicol. 2003;16:1070-7 pubmed
    ..Liver mRNA was isolated from rats dosed with six different chemicals, dexamethasone, troleandomycin, miconazole, clotrimazole, and methylclofanapate, which are all known to induce different cytochrome P450 ..
  42. DiPetrillo K, Wood S, Kostrubsky V, Chatfield K, Bement J, Wrighton S, et al. Effect of caffeine on acetaminophen hepatotoxicity in cultured hepatocytes treated with ethanol and isopentanol. Toxicol Appl Pharmacol. 2002;185:91-7 pubmed
    ..The results indicate that CYP3A is responsible for the caffeine-mediated stimulation of APAP toxicity. Our results suggest that caffeine may be an additional risk factor for developing alcohol-mediated APAP hepatotoxicity. ..
  43. van t Klooster G, Horbach G, Natsuhori M, Blaauboer B, Noordhoek J, Van Miert A. Hepatic cytochrome P450 induction in goats. Effects of model inducers on the metabolism of alkoxyresorufins, testosterone and ethylmorphine, and on apoprotein and mRNA levels. Biochem Pharmacol. 1993;45:113-22 pubmed
    ..With BNF-treated animals, increased concentrations of a protein cross-reactive with anti-rat P450 1A1/1A2 and of an mRNA that showed homology with a human 1A1 cDNA probe, but not with a mouse 1A1/1A2 probe, were observed. ..
  44. McNamee J, Kobus S, Marks G. The apoprotein of cytochrome P450 3A2 does not selectively direct alkylation to one of four pyrrole rings of N-vinylprotoporphyrin IX. Can J Physiol Pharmacol. 1996;74:996-1000 pubmed
    ..Following coadministration of TTMS with troleandomycin, N-vinylPP formation is reduced to 40 and 43% of control in untreated and dexamethasone-pretreated male rats...
  45. Yasar U, Annas A, Svensson J, Lazorova L, Artursson P, Al Shurbaji A. Ketobemidone is a substrate for cytochrome P4502C9 and 3A4, but not for P-glycoprotein. Xenobiotica. 2005;35:785-96 pubmed
    ..The data suggest that CYP2C9 and CYP3A4 play a major role in the formation of norketobemidone at clinically relevant concentrations. ..
  46. Szucs G, Tamasi V, Laczay P, Monostory K. Biochemical background of toxic interaction between tiamulin and monensin. Chem Biol Interact. 2004;147:151-61 pubmed
    ..The direct effect of tiamulin as an inhibitor might play a more important role in toxicity than its putative effect as a chemical inducer of CYP3A enzymes. ..
  47. Reilly P, Mason S, Read M. Human, rat and crocodile liver microsomal monooxygenase activities measured using diazepam and nifedipine: effects of CYP3A inhibitors and relationship to immunochemically detected CYP3A apoprotein. Comp Biochem Physiol C Pharmacol Toxicol Endocrinol. 1999;122:197-204 pubmed
    ..These results show the need for care in the assessment of CYP3A activity of fractionated tissues when using these substrates in cross-species studies and where gender is a variable. ..
  48. Kharasch E, Walker A, Hoffer C, Sheffels P. Intravenous and oral alfentanil as in vivo probes for hepatic and first-pass cytochrome P450 3A activity: noninvasive assessment by use of pupillary miosis. Clin Pharmacol Ther. 2004;76:452-66 pubmed
    ..crossover design after administration of rifampin (INN, rifampicin) (hepatic and intestinal CYP3A induction), troleandomycin (TAO) (hepatic and intestinal CYP3A inhibition), grapefruit juice (selective intestine CYP3A inhibition), or ..
  49. Lee J, Kim E, Kwon J, Yoo M, Lee M. Negligible pharmacokinetic interaction between oral DA-8159, a new erectogenic, and amlodipine in rats. Biopharm Drug Dispos. 2006;27:125-31 pubmed
    ..In rats pretreated with troleandomycin (a main inhibitor of CYP3A1/2 in rats), the AUC(0-6 h) of amlodipine was significantly greater than the ..
  50. McGinnity D, Berry A, Kenny J, Grime K, Riley R. Evaluation of time-dependent cytochrome P450 inhibition using cultured human hepatocytes. Drug Metab Dispos. 2006;34:1291-300 pubmed
    ..were determined after incubation with the prototypic inhibitors tienilic acid (CYP2C9), erythromycin, troleandomycin, and fluoxetine (CYP3A4)...
  51. Lake B, Renwick A, Cunninghame M, Price R, Surry D, Evans D. Comparison of the effects of some CYP3A and other enzyme inducers on replicative DNA synthesis and cytochrome P450 isoforms in rat liver. Toxicology. 1998;131:9-20 pubmed
    ..CLOT), 75 mg/kg per day methylclofenapate (MCP), 50 mg/kg per day dexamethasone (DEX) and 500 mg/kg per day troleandomycin (TAO) by daily oral gavage for four days...
  52. Wang H, Peng R, Zhang Y, Chen J, Li Q, Kong R, et al. Demethylation capacity of human fetal adrenal mitochondrial cytochrome P-450 in vitro. Zhongguo Yao Li Xue Bao. 1999;20:358-62 pubmed
    ..708, P < 0.05) and benzfetamine (r = 0.707, P < 0.05). Troleandomycin stimulated erythromycin N-demethylation in adrenal mitochondria as well as in adrenal and liver microsomes in ..
  53. Ray W, Murray K, Meredith S, Narasimhulu S, Hall K, Stein C. Oral erythromycin and the risk of sudden death from cardiac causes. N Engl J Med. 2004;351:1089-96 pubmed
    ..The CYP3A inhibitors used in the study were nitroimidazole antifungal agents, diltiazem, verapamil, and troleandomycin; each doubles, at least, the area under the time-concentration curve for a CYP3A substrate...