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Telithromycin

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Chemistry

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Also known as: Ketek, 191114-48-4, Hmr 3647, Levviax, Hmr-3647, Hmr3647

Molecular Formula

C₄₃H₆₅N₅O₁₀

Molecular Weight

812.0 g/mol

InChI Key

LJVAJPDWBABPEJ-PNUFFHFMSA-N

FDA UNII

KI8H7H19WL

Telithromycin, a semi-synthetic erythromycin derivative, belongs to a new chemical class of antibiotics called ketolides. Ketolides have been recently added to the macrolide-lincosamide-streptogramin class of antibiotics. Similar to the macrolide antibiotics, telithromycin prevents bacterial growth by interfering with bacterial protein synthesis. Telithromycin binds to the 50S subunit of the 70S bacterial ribosome and blocks further peptide elongation. Binding occurs simultaneously at to two domains of 23S RNA of the 50S ribosomal subunit, domain II and V, where older macrolides bind only to one. It is used to treat mild to moderate respiratory infections.

Telithromycin is a Ketolide Antibacterial.

1 2D Structure

Telithromycin

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(1S,2R,5R,7R,8R,9R,11R,13R,14R)-8-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-15-[4-(4-pyridin-3-ylimidazol-1-yl)butyl]-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone

2.1.2 InChI

InChI=1S/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

2.1.3 InChI Key

LJVAJPDWBABPEJ-PNUFFHFMSA-N

2.1.4 Canonical SMILES

CCC1C2(C(C(C(=O)C(CC(C(C(C(=O)C(C(=O)O1)C)C)OC3C(C(CC(O3)C)N(C)C)O)(C)OC)C)C)N(C(=O)O2)CCCCN4C=C(N=C4)C5=CN=CC=C5)C

2.1.5 Isomeric SMILES

CC[C@@H]1[C@@]2([C@@H]([C@H](C(=O)[C@@H](C[C@@]([C@@H]([C@H](C(=O)[C@H](C(=O)O1)C)C)O[C@H]3[C@@H]([C@H](C[C@H](O3)C)N(C)C)O)(C)OC)C)C)N(C(=O)O2)CCCCN4C=C(N=C4)C5=CN=CC=C5)C

2.2 Other Identifiers

2.2.1 UNII

KI8H7H19WL

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Hmr 3647

2. Hmr-3647

3. Hmr3647

4. Ketek

5. Ru 66647

6. Ru-66647

2.3.2 Depositor-Supplied Synonyms

1. Ketek

2. 191114-48-4

3. Hmr 3647

4. Levviax

5. Hmr-3647

6. Hmr3647

7. Ru-66647

8. Ki8h7h19wl

9. Nsc-758940

10. Dsstox_cid_26455

11. Dsstox_rid_81629

12. Dsstox_gsid_46455

13. 2h-oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(1h,7h,9h)-tetrone, 4-ethyloctahydro-11-methoxy-3a,7,9,11,13,15-hexamethyl-1-[4-[4-(3-pyridinyl)-1h-imidazol-1-yl]butyl]-10-[[3,4,6-trideoxy-3-(dimethylamino)-beta-d-xylo-hexopyranosyl]oxy]-, (3as,4r,7r,9r,10r,11r,13r,15r,15ar)-

14. Ru 66647

15. Ru66647

16. Cas-191114-48-4

17. Unii-ki8h7h19wl

18. Telithromycin [usan:inn:ban]

19. Hsdb 7359

20. Ncgc00164575-01

21. Telithromycin [mi]

22. Telithromycin [inn]

23. Telithromycin [jan]

24. Schembl5100

25. Chembl1136

26. Telithromycin [hsdb]

27. Telithromycin [usan]

28. Telithromycin [vandf]

29. Telithromycin [mart.]

30. Telithromycin [who-dd]

31. Dtxsid3046455

32. Telithromycin [ema Epar]

33. Chebi:29688

34. Telithromycin [orange Book]

35. Hy-a0062

36. Zinc9574770

37. Tox21_111454

38. Tox21_112203

39. Bdbm50378137

40. Mfcd00943561

41. Db00976

42. Nsc 758940

43. Hmr-3647;ru-66647

44. 11,12-dideoxy-3-des(2,6-dideoxy-3-c,3-o-dimethyl-alpha-l-altropyranosyloxy)-6-o-methyl-3-oxo-12,11-(oxycarbonylimino)-n11-[4-[4-(3-pyridyl)imidazol-1-yl]butyl]erythromycin A

45. Q2736135

46. (1r,2r,4r,6r,7r,8r,10r,13r,14s)-7-[(2s,3r,4s,6r)-4-(dimethylamino)-3-hydroxy-6-methyl-tetrahydropyran-2-yl]oxy-13-ethyl-6-methoxy-2,4,6,8,10,14-hexamethyl-17-[4-[4-(3-pyridyl)imidazol-1-yl]butyl]-12,15-dioxa-17-azabicyclo[12.3.0]heptadecane-3,9,11,16-tetrone

47. (1s,2r,5r,7r,8r,9r,11r,13r,14r)-8-[(2s,3r,4s,6r)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-15-[4-(4-pyridin-3-ylimidazol-1-yl)butyl]-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone

48. (3as,4r,7r,9r,10r,11r,13r,15r,15ar)-4-ethyl-11-methoxy-3a,7,9,11,13,15-hexamethyl-1-(4-(4-(pyridin-3-yl)-1h-imidazol-1-yl)butyl)-10-((3,4,6-trideoxy-3-(dimethylamino)-b-d-xylo-hexopyranosyl)oxy)octahydro-2h-oxacyclotetradecino(4,3-d)oxazole-2,6,8,14(1h,7h,9h)-tetrone

49. (3as,4r,7r,9r,10r,11r,13r,15r,15ar)-4-ethyl-11-methoxy-3a,7,9,11,13,15-hexamethyl-2,6,8,14-tetraoxo-1-{4-[4-(pyridin-3-yl)-1h-imidazol-1-yl]butyl}tetradecahydro-2h-oxacyclotetradecino[4,3-d][1,3]oxazol-10-yl 3,4,6-trideoxy-3-(dimethylamino)-beta-d-xylo-hexopyranoside

50. Erythromycin, 3-de((2,6-dideoxy-3-c-methyl-3-o-methyl-alpha-l-ribo-hexopyranosyl)oxy)-11,12-dideoxy-6-o-methyl-3-oxo-12,11-(oxycarbonyl((4-(4-(3-pyridinyl)-1h-imidazol-1-yl)butyl)imino))-

51. Erythromycin, 3-de[(2,6-dideoxy-3-c-methyl-3-o-methyl-.alpha.-l-ribo-hexopyranosyl)oxy]-11,12-dideoxy-6-o-methyl-3-oxo-12,11-[oxycarbonyl[[4-[4-(3-pyridinyl)-1h-imidazol-1-yl]butyl]imino]]-

52. Erythromycin,3-de((2,6-dideoxy-3-c-methyl-3-o-methyl-.alpha.-l-ribo-hexopyranosyl)oxy)-11,12-dideoxy-6-o-methyl-3-oxo-12,11-(oxycarbonyl((4-(4-(3-pyridinyl)-1h-imidazol-1-yl)butyl)imino)-

2.4 Create Date

2005-06-24

3 Chemical and Physical Properties

Molecular Formula	C₄₃H₆₅N₅O₁₀
Molecular Weight	812.0 g/mol
XLogP3	4.2
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	13
Rotatable Bond Count	11
Exact Mass	811.47314329 g/mol
Monoisotopic Mass	811.47314329 g/mol
Topological Polar Surface Area	172 Å²
Heavy Atom Count	58
Formal Charge	0
Complexity	1440
Isotope Atom Count	0
Defined Atom Stereocenter Count	13
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Information

1 of 2
Drug Name	Ketek
PubMed Health	Telithromycin (By mouth)
Drug Classes	Antibiotic
Drug Label	KETEK tablets contain telithromycin, a semisynthetic antibacterial in the ketolide class for oral administration. Chemically, telithromycin is designated as Erythromycin, 3-de[(2,6-dideoxy-3-C-methyl-3-O-methyl--L-ribo-hexopyranosyl)oxy]-11,12-di...
Active Ingredient	Telithromycin
Dosage Form	Tablet
Route	Oral
Strength	400mg; 300mg
Market Status	Prescription
Company	Sanofi Aventis Us

2 of 2
Drug Name	Ketek
PubMed Health	Telithromycin (By mouth)
Drug Classes	Antibiotic
Drug Label	KETEK tablets contain telithromycin, a semisynthetic antibacterial in the ketolide class for oral administration. Chemically, telithromycin is designated as Erythromycin, 3-de[(2,6-dideoxy-3-C-methyl-3-O-methyl--L-ribo-hexopyranosyl)oxy]-11,12-di...
Active Ingredient	Telithromycin
Dosage Form	Tablet
Route	Oral
Strength	400mg; 300mg
Market Status	Prescription
Company	Sanofi Aventis Us

4.2 Therapeutic Uses

Antibacterial

O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. 13th Edition, Whitehouse Station, NJ: Merck and Co., Inc., 2001., p. 1627

Telithromycin in indicated in the treatment of acute bacterial exacerbation of chronic bronchitis due to Streptococcus pneumoniae, Haemophilus influenzae, or Moraxella catarrhalis. /Included in US product labeling/

Thomson.Micromedex. Drug Information for the Health Care Professional. 25th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2005., p. 2726

Telithromycin is indicated for the treatment of group A-beta Hemolytic Streptococcus as an alternative when beta-lactam antibiotics are not appropriate. /NOT included in US product labeling/

Telithromycin is indicated in the treatment of community-acquired pneumonia due to Streptococcus pneumoniae (including multi-drug resistant isolates (MDRSP)), Haemophilus influenzae, Chlamydophila pneumoniae, Mycoplasma pneumoniae, or Moraxella catarrhalis. /NOT included in US product labeling/

Telithromycin is indicated in the treatment of acute bacterial sinusitis due to Steptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, or Staphylococcus aureus. /Included in US product labeling/

4.3 Drug Warning

Pseudomembranous colitis has been reported with nearly all antibacterial agents, including telithromycin, and may range in severity from mild to life-threatening. Therefore, it is important to consider this diagnosis in patients who present with diarrhea subsequent to the administration of any antibacterial agents.

Physicians Desk Reference. 59th ed. Thomson PDR. Montvale, NJ 2005., p. 711

FDA Pregnancy Risk Category: C /RISK CANNOT BE RULED OUT. Adequate, well controlled human studies are lacking, and animal studies have shown risk to the fetus or are lacking as well. There is a chance of fetal harm if the drug is given during pregnancy; but the potential benefits may outweigh the potential risk./

Treatment with anti-infectives, including telithromycin, may permit overgrowth of clostridia. Consider Clostridium difficile-associated diarrhea and colitis (antibiotic-associated pseudomembranous colitis) if diarrhea develops and manage accordingly. Some mild cases of C. difficile-asssociated diarrhea and colitis may respond to discontinuance alone. Manage moderate to severe cases with fluid, electrolyte, and protein supplementation; appropriate anti-infective therapy (e.g., oral metronidazole or vancomycin) recommended if colitis is severe

McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 231

To reduce development of drug-resistant bacteria and maintain effectiveness of telithromycin and other antibacterials, use only for treatment of infections proven or strongly suspected to be caused by susceptible bacteria. When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing. In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.

McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 232

For more Drug Warnings (Complete) data for TELITHROMYCIN (14 total), please visit the HSDB record page.

4.4 Drug Indication

For the treatment of Pneumococcal infection, acute sinusitis, acute bacterial tonsillitis, acute bronchitis and bronchiolitis, lower respiratory tract infection and lobar (pneumococcal) pneumonia.

FDA Label

When prescribing Ketek, consideration should be given to official guidance on the appropriate use ofantibacterial agents and the local prevalence of resistance.

Ketek is indicated for the treatment of the following infections:

* In patients of 18 years and older:

- community-acquired pneumonia, mild or moderate.

- when treating infections caused by known or suspected beta-lactam- and / or macrolide-resistant strains (according to history of patients or national and / or regional resistance data) covered by the antibacterial spectrum of telithromycin:

- acute exacerbation of chronic bronchitis;

- acute sinusitis;

* In patients of 12 years and older:

- tonsillitis / pharyngitis caused by Streptococcus pyogenes, as an alternative when beta-lactam antibiotics are not appropriate in countries / regions with a significant prevalence of macrolide-resistant S. pyogenes, when mediated by ermTR or mefA.

When prescribing Levviax consideration should be given to official guidance on the appropriate use of antibacterial agents and the local prevalence of resistance (see also sections 4. 4 and 5. 1).

Levviax is indicated for the treatment of the following infections:

In patients of 18 years and older:

-Community-acquired pneumonia, mild or moderate (see section 4. 4).

- When treating infections caused by known or suspected beta-lactam and/or macrolide resistant strains (according to history of patients or national and/or regional resistance data) covered by the antibacterial spectrum of telithromycin (see sections 4. 4 and 5. 1):

- Acute exacerbation of chronic bronchitis,

- Acute sinusitis

In patients of 12 years and older:

- Tonsillitis/pharyngitis caused by Streptococcus pyogenes, as an alternative when beta lactam antibiotics are not appropriate in countries/regions with a significant prevalence of macrolide resistant S. pyogenes, when mediated by ermTR or mefA (see sections 4. 4 and 5. 1).

5 Pharmacology and Biochemistry

5.1 Pharmacology

Telithromycin is a ketolide antibiotic which has an antimicrobial spectrum similar or slightly broader than that of penicillin. It is often used as an alternative in patients who have an allergy to penicillins. For respiratory tract infections, it has better coverage of atypical organisms, including mycoplasma. Telithromycin prevents bacterial growth by binding to bacterial 50S ribosomal subunits and interfering with bacterial peptide translocation and elongation.

5.2 MeSH Pharmacological Classification

Anti-Bacterial Agents

Substances that inhibit the growth or reproduction of BACTERIA. (See all compounds classified as Anti-Bacterial Agents.)

5.3 FDA Pharmacological Classification

5.3.1 Active Moiety

TELITHROMYCIN

5.3.2 FDA UNII

KI8H7H19WL

5.3.3 Pharmacological Classes

Chemical Structure [CS] - Ketolides

5.4 ATC Code

J01FA15

J - Antiinfectives for systemic use

J01 - Antibacterials for systemic use

J01F - Macrolides, lincosamides and streptogramins

J01FA - Macrolides

J01FA15 - Telithromycin

5.5 Absorption, Distribution and Excretion

Absorption

Absolute bioavailability is approximately 57%. Maximal concentrations are reached 0.5 - 4 hours following oral administration. Food intake does not affected absorption.

Route of Elimination

The systemically available telithromycin is eliminated by multiple pathways as follows: 7% of the dose is excreted unchanged in feces by biliary and/or intestinal secretion; 13% of the dose is excreted unchanged in urine by renal excretion; and 37% of the dose is metabolized by the liver.

Volume of Distribution

2.9 L/kg

Telithromycin concentration in white blood cells exceeds the concentration in plasma and is eliminated more slowly from white blood cells than from plasma. Mean white blood cell concentrations of telithromycin peaked at 72.1 ug/mL at 6 hours, and remained at 14.1 ug/mL 24 hours after 5 days of repeated dosing of 600 mg once daily. After 10 days, repeated dosing of 600 mg once daily, white blood cell concentrations remained at 8.9 ug/mL 48 hours after the last dose.

Physicians Desk Reference. 59th ed. Thomson PDR. Montvale, NJ 2005., p. 710

Volume of distribution - 2.9 L/kg following an intervenous infusion. Widely distributed throughout the body. Telithromycin is distributed into breast milk of rats.

Rapidly absorbed, absolute bioavailability is 57% in both young and elderly patients. The rate and extent of absorption are unaffected by food. The AUC following a single dose is 8.25 ug h/mL and 12.5 ug h/mL following multiple dosing.

Physicians Desk Reference. 59th ed. Thomson PDR. Montvale, NJ 2005., p. 710

For more Absorption, Distribution and Excretion (Complete) data for TELITHROMYCIN (11 total), please visit the HSDB record page.

5.6 Metabolism/Metabolites

Hepatic - estimated 50% metabolized by CYP3A4 and 50% metabolized independent of cytochrome P450

About 70% (33% presystemic and 37% systemic) of an oral dose is metabolized about equally by cytochrome P450 (CYP) 3A4 and non-CYP3A4 isoenzymes to 4 major metabolites. The systemically available telithromycin is eliminated in the feces as unchanged drug (7%), in urine as unchanged drug (13%), and 37% is metabolized in the liver.

McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 233

Biotransformation: Hepatic; 37% of the dose is metabolized by the liver. Metabolism accounts for approximately 70% of the dose. The main metabolite represented 12.6% of the AUC while three other metabolites quantified represented 3% or less of the AUC of telithromycin.

In total, metabolism accounts for approximately 70% of the dose. In plasma, the main circulating compound after administration of an 800-mg radiolabeled dose was parent compound, representing 56.7% of the total radioactivity. The main metabolite represented 12.6% of the AUC of telithromycin. Three other plasma metabolites were quantified, each representing 3% or less of the AUC of telithromycin. It is estimated that approximately 50% of its metabolism is mediated by CYP 450 3A4 and the remaining 50% is CYP 450-independent.

Physicians Desk Reference. 59th ed. Thomson PDR. Montvale, NJ 2005., p. 710

5.7 Biological Half-Life

Main elimination half-life is 2-3 hours; terminal elimination half-life is 10 hours

Elimination: 10 hours following oral dosing.

5.8 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 binding site at domain V. Telithromycin may also inhibit the assembly of nascent ribosomal units. Compared to erythromycin A, telithromycin binds to the 23S rRNA with 10 times greater affinity in erythromycin-susceptible organisms and 25 times greater affinity in macrolide-resistant strains. This increased binding affinity may be conferred by the C11-12 carbamate side chain of telithromycin. The side chain appears to maintain binding at domain II in the presence of resistance mediated by alterations in domain V.

Telithromycin may be bacteriostatic or bactericidal in action. Like conventional macrolides, telithromycin inhibits protein synthesis in susceptible organisms by binding to the 50S ribosomal subunit. Telithromycin binds to domains II and V of the 23S rRNA of the 50S subunit and has a higher affinity for these ribosomal targets than conventional macrolides, apparently because of additional interactions and increased binding at domain II. This allows telithromycin to retain activity against some gram-positive cocci (e.g., some strains ofS. pneumoniae) that have methylase-mediated resistance (erm genes) that alter the domain V binding site. In addition to inhibiting protein synthesis, telithromycin may inhibit assembly of nascent ribosomal units.

McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 233

Telithromycin blocks protein synthesis by binding to two sites on the 50S ribosomal subunit: domain II and V of the 23S rRNA. The greater affinity in binding strength can be attributed to the C11-C12 carbamate side chain.

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