TELITHROMYCIN

US Previously Marketed

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C43H65N5O10
Molecular Weight	812.0037
Optical Activity	UNSPECIFIED
Defined Stereocenters	13 / 13
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=LJVAJPDWBABPEJ-PNUFFHFMSA-N

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

HIDE SMILES / InChI

Molecular Formula	C43H65N5O10
Molecular Weight	812.0037
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	13 / 13
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21144_ketek_lbl.pdf
Curator's Comment: description was created based on several sources, including: http://www.drugbank.ca/drugs/DB00976 https://en.wikipedia.org/wiki/Telithromycin

French pharmaceutical company Hoechst Marion Roussel (later Sanofi-Aventis) began phase II/III clinical trials of telithromycin (HMR-3647) in 1998. Telithromycin was approved by the European Commission in July 2001 and subsequently went on sale in October 2001. In the US, telithromycin received U.S. Food and Drug Administration (FDA) approval on April 1, 2004 Telithromycin is the first ketolide antibiotic to enter clinical use and is sold under the brand name of Ketek. After significant controversy regarding safety and research fraud, the US Food and Drug Administration sharply curtailed the approved uses of the drug in 2007. Telithromycin is a semi-synthetic erythromycin derivative. It is created by substituting a ketogroup for the cladinose sugar and adding a carbamate ring in the lactone ring. An alkyl-aryl moiety is attached to this carbamate ring. Furthermore, the carbon at position 6 has been methylated, as is the case in clarithromycin, to achieve better acid-stability. For the treatment of Pneumococcal infection, acute sinusitis, acute bacterial tonsillitis, acute bronchitis and bronchiolitis, lower respiratory tract infection and lobar (pneumococcal) pneumonia. KETEK tablets contain telithromycin, a semisynthetic antibacterial in the ketolide class for oral administration. Telithromycin blocks protein synthesis 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.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Bacterial 70S ribosome 179 Target ID: CHEMBL2363135 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21144_ketek_lbl.pdf	Inhibitor 8297

Conditions

Condition	Modality	Highest Phase	Product
Community-acquired pneumonia 47 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21144_ketek_lbl.pdf	Curative	Approved 8429	KETEK Approved Use KETEK tablets are indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the conditions listed below for patients 18 years old and above. Launch Date 2004
Acute bacterial exacerbation of chronic bronchitis 31 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21144_ketek_lbl.pdf	Curative	Approved 8429	KETEK Approved Use KETEK tablets are indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the conditions listed below for patients 18 years old and above. Launch Date 2004
Acute bacterial sinusitis 26 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21144_ketek_lbl.pdf	Curative	Approved 8429	KETEK Approved Use KETEK tablets are indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the conditions listed below for patients 18 years old and above. Launch Date 2004

C_max

Value	Dose	Analyte	Population
2.27 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.8 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.07 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	1600 mg single, oral dose: 1600 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.829 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.48 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	1600 mg 1 times / day steady-state, oral dose: 1600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.9 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.27 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021144s012lbl.pdf	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.9 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021144s012lbl.pdf	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
12.5 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.57 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
23.1 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	1600 mg single, oral dose: 1600 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.5 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
30.2 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	1600 mg 1 times / day steady-state, oral dose: 1600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8.25 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.5 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021144s012lbl.pdf	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
8.25 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021144s012lbl.pdf	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
9.81 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.68 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10.13 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	1600 mg single, oral dose: 1600 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	1600 mg 1 times / day steady-state, oral dose: 1600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.16 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11120961/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.81 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021144s012lbl.pdf	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
7.16 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021144s012lbl.pdf	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
35% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021144s012lbl.pdf	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:		TELITHROMYCIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
800 mg 1 times / day multiple, oral Recommended Dose: 800 mg, 1 times / day Route: oral Route: multiple Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12749505 Page: p.436	unhealthy, 13-72 n = 232 Health Status: unhealthy Condition: Group A beta-hemolytic streptococcal tonsillitis/pharyngitis Age Group: 13-72 Sex: M+F Population Size: 232 Sources: https://pubmed.ncbi.nlm.nih.gov/12749505 Page: p.436	Disc. AE: Allergic reaction, Alanine aminotransferase increase... AEs leading to discontinuation/dose reduction: Allergic reaction Alanine aminotransferase increase Aspartate aminotransferase increase Lactate dehydrogenase increased Sources: https://pubmed.ncbi.nlm.nih.gov/12749505 Page: p.436
800 mg 1 times / day multiple, oral Recommended Dose: 800 mg, 1 times / day Route: oral Route: multiple Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16611950 Page: p.1598	unhealthy, 17–64 n = 140 Health Status: unhealthy Condition: asthma Age Group: 17–64 Sex: M+F Population Size: 140 Sources: https://pubmed.ncbi.nlm.nih.gov/16611950 Page: p.1598	Other AEs: Diarrhea, Nausea... Other AEs: Diarrhea (9.8%) Nausea (5.3%) Nausea (3.8%) Sources: https://pubmed.ncbi.nlm.nih.gov/16611950 Page: p.1598
1600 mg 1 times / day multiple, oral Highest studied dose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/11120961 Page: p.173	healthy, 18 -45 n = 18 Health Status: healthy Age Group: 18 -45 Sex: M Population Size: 18 Sources: https://pubmed.ncbi.nlm.nih.gov/11120961 Page: p.173	Disc. AE: Vomiting, Diarrhea... AEs leading to discontinuation/dose reduction: Vomiting (grade 3, 5.6%) Diarrhea (grade 3, 5.6%) Sources: https://pubmed.ncbi.nlm.nih.gov/11120961 Page: p.173
2400 mg single, oral Highest studied dose Dose: 2400 mg Route: oral Route: single Dose: 2400 mg Sources: https://pubmed.ncbi.nlm.nih.gov/12621389 Page: p.250	healthy, 18-35 n = 16 Health Status: healthy Age Group: 18-35 Sex: M+F Population Size: 16 Sources: https://pubmed.ncbi.nlm.nih.gov/12621389 Page: p.250	Other AEs: Nausea, Diarrhea... Other AEs: Nausea (grade 1-2) Diarrhea (grade 1-2) Abdominal pain (grade 1-2) Headache (grade 1-2) Taste disturbance (grade 1-2) Dizziness (grade 1-2) Sources: https://pubmed.ncbi.nlm.nih.gov/12621389 Page: p.250
800 mg 1 times / day multiple, oral Recommended Dose: 800 mg, 1 times / day Route: oral Route: multiple Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/14996517 Page: p.57	unhealthy, 18-83 n = 224 Health Status: unhealthy Condition: Community-acquired pneumonia Age Group: 18-83 Sex: M+F Population Size: 224 Sources: https://pubmed.ncbi.nlm.nih.gov/14996517 Page: p.57	Disc. AE: Vomiting, Nausea... Other AEs: Headache, Taste perversion... AEs leading to discontinuation/dose reduction: Vomiting (grade 3, 1.4%) Nausea (grade 3, 0.45%) Alanine aminotransferase increase (grade 3, 0.45%) Aspartate aminotransferase increase (grade 3, 0.45%) Other AEs: Headache (4.1%) Taste perversion (3.6%) Diarrhea (12.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/14996517 Page: p.57
800 mg 1 times / day multiple, oral Recommended Dose: 800 mg, 1 times / day Route: oral Route: multiple Dose: 800 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021144s013lbl.pdf Page: p.12	unhealthy Health Status: unhealthy Condition: Community-acquired pneumonia Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021144s013lbl.pdf Page: p.12	Other AEs: Acute hepatic failure, Liver injury... Other AEs: Acute hepatic failure (grade 4-5) Liver injury (grade 4-5) Hepatitis fulminant (grade 4) Hepatic necrosis (grade 4) Hepatic enzymes increased (grade 2) Hepatitis (grade 2) Jaundice (grade 2) Electrocardiogram QTc interval prolonged Visual disturbances Blurred vision Diplopia Loss of consciousness Vagal reaction Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021144s013lbl.pdf Page: p.12

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587		inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1461 OATP1B1 788 OATP1B3 706	P-gp 1537

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2004/21-144_Ketek_BioPharmr_P1.pdf#page=33 Page: 33.0	weak	weak (co-administration study) Comment: Co-administration of telithromycin increased the bioavailability of metropolol resulted in in ~1.4 fold increase in both AUC and Cmax; there was no pharmacokinetic effect on paroxetine Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2004/21-144_Ketek_BioPharmr_P1.pdf#page=33 Page: 33.0
P-gp 1650	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/18027988/	yes [IC50 1.8 uM]
OATP1B3 715	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/17296622/	yes [IC50 11 uM]
OATP1B1 803	inhibitor 3277 Sources: https://dmd.aspetjournals.org/content/early/2018/10/22/dmd.118.083832	yes [IC50 12 uM]
CYP3A4 1925	inhibitor 3277 Sources: https://dmd.aspetjournals.org/content/early/2018/10/22/dmd.118.083832	yes [Ki 3.65 uM]	yes (co-administration study) Comment: Cisapride: Steady-state peak plasma concentrations of cisapride (an agent with the potential to increase QT interval) were increased by 95% when co-administered with repeated doses of telithromycin; Simvastatin: When simvastatin was co-administered with telithromycin, there was a 5.3-fold increase in simvastatin Cmax, an 8.9-fold increase in simvastatin AUC, a 15-fold increase in the simvastatin active metabolite Cmax, and a 12-fold increase in the simvastatin active metabolite AUC; Midazolam: Concomitant administration of telithromycin with intravenous or oral midazolam resulted in 2- and 6-fold increases, respectively, in the AUC of midazolam due to inhibition of CYP 3A4- dependent metabolism of midazolam; Sources: https://dmd.aspetjournals.org/content/early/2018/10/22/dmd.118.083832

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 1537	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1346787/	yes
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21144_ketek_lbl.pdf#page=3 Page: 3.0	yes		yes (co-administration study) Comment: Itraconazole: A multiple-dose interaction study with itraconazole showed that Cmax of telithromycin was increased by 22% and AUC by 54%; Ketoconazole: A multiple-dose interaction study with ketoconazole showed that Cmax of telithromycin was increased by 51% and AUC by 95%; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21144_ketek_lbl.pdf#page=3 Page: 3.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://pubmed.ncbi.nlm.nih.gov/16614168/

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY535749	https://www.001chemical.com/chem/191114-48-4
AA Blocks	AA002EZ0	https://www.aablocks.com/goods/Goods/detail?id=AA002EZ0
AK Scientific, Inc. (AKSCI)	69309	http://www.aksci.com/item_detail.php?cat=69309
AbMole Bioscience	M9301	http://www.abmole.com/products/telithromycin.html
Alfa Chemistry	AP191114484	https://reagents.alfa-chemistry.com/product/telithromycin-cas-191114-48-4-7099.html
Angene	AGN-PC-0WH20M	http://www.angenechemical.com/productshow/AGN-PC-0WH20M.html
Aurora Fine Chemicals LLC	A24.091.186	http://online.aurorafinechemicals.com/info?ID=A24.091.186
BOC Sciences	191114-48-4	https://www.bocsci.com/product/telithromycin-cas-191114-48-4-61930.html
BOC Sciences	173838-31-8	https://www.bocsci.com/telithromycin-cas-173838-31-8-item-186731.html
BioChemPartner	BCP08211	http://www.biochempartner.com/191114-48-4-BCP08211
BioCrick	BCC5273	http://www.biocrick.com/Telithromycin-BCC5273.html
BioSynth	T-1460	https://www.biosynth.com/products/biochemistry/culture-media-additives/products/T-1460.html
Boerchem	BC208806	http://www.boerchem.com/?product_35327.html
Chem Scene	CS-2812	http://www.chemscene.com/191114-48-4.html
ChemMol	30104415	http://www.chemmol.com/chemmol/30104415.html
ChemMol	44003358	http://www.chemmol.com/chemmol/44003358.html
ChemMol	49408552	http://www.chemmol.com/chemmol/49408552.html
Chemspace	CSSB00161189708	https://chem-space.com/CSSB00161189708
DC Chemicals	DCAPI1102	http://www.dcchemicals.com//product_show-Telithromycin_Ketek_.html
Finetech	FT-0674835	http://www.finetechnology-ind.com/prod/detail/pub/191114-48-4.html
Glentham Life Sciences	GA2425	http://www.glentham.com/products/product/GA2425/
Hairui	HR131121	http://www.hairuichem.com/en/product/191114-48-4.html
Lab Network	LN01343501	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01343501
MedChem Express	HY-A0062	https://www.medchemexpress.com/telithromycin.html
MetabolomicsWorkbench	71351	http://www.metabolomicsworkbench.org/data/StructureData.php?RegNo=71351
MolPort	MolPort-023-220-177	https://www.molport.com/shop/molecule-link/MolPort-023-220-177
Molcore	MC535749	https://www.molcore.com/product/191114-48-4
OChem	24626	http://www.ocheminc.com/index.php?act=psearch&pid=114T484
Sinfoo Biotech	S055721	http://www.sinfoobiotech.com/product/1059119
Smolecule	S544869	http://www.smolecule.com/products/s544869
Smolecule	S720045	https://www.smolecule.com/products/s720045
THE BioTek	bt-283987	https://www.thebiotek.com/product/inhibitors/bt-283987
Vesino Industrial Co Ltd	VA11985	http://www.vsnchem.com/goto/product/22286/
W&J PharmaChem	100667	http://www.wjpharmachem.com/new/100667.html
Yuhao Chemical	HL3816	http://www.chemyuhao.com/191114-48-4.html
abcr GmbH	AB479656	http://www.abcr.com/shop/en/AB479656

PubMed

Title	Date	PubMed
The ketolide antibiotics HMR 3647 and HMR 3004 are active against Toxoplasma gondii in vitro and in murine models of infection.	1997 Oct	9333038
Use of ketolides in combination with other drugs to treat experimental toxoplasmosis.	1998 Nov	9848454
In vitro susceptibilities of rapidly growing mycobacteria to telithromycin (HMR 3647) and seven other antimicrobials.	2000 Jan	10602744
In vitro activities of the ketolides telithromycin (HMR 3647) and HMR 3004 compared to those of clarithromycin against slowly growing mycobacteria at pHs 6.8 and 7.4.	2000 Oct	10991870
Telithromycin is active against Mycobacterium avium in mice despite lacking significant activity in standard in vitro and macrophage assays and is associated with low frequency of resistance during treatment.	2001 Aug	11451676
Telithromycin-induced acute interstitial nephritis: a first case report.	2004 Aug	15264209
In vitro and in vivo activities of macrolide derivatives against Mycobacterium tuberculosis.	2005 Apr	15793125
Verapamil toxicity resulting from a probable interaction with telithromycin.	2005 Feb	15598962
Pill esophagitis caused by telithromycin: a case report.	2006 Jun	16830293
Acute hepatitis attack after exposure to telithromycin.	2007 Aug	17919553
Cellular imaging predictions of clinical drug-induced liver injury.	2008 Sep	18524759
Synergistic drug-cytokine induction of hepatocellular death as an in vitro approach for the study of inflammation-associated idiosyncratic drug hepatotoxicity.	2009 Jun 15	19362101
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.	2010 Dec	20829430
Effect of telithromycin on the pharmacokinetics and pharmacodynamics of oral oxycodone.	2010 Jan	19755414
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.	2013 Nov	23956101
Utilization of human nuclear receptors as an early counter screen for off-target activity: a case study with a compendium of 615 known drugs.	2015 Jun	25752796

Patents

Sample Use Guides

In Vivo Use Guide

800 mg taken orally once every 24 hours

Route of Administration: Oral

In Vitro Use Guide

The clinical isolates tested were an erythromycinsusceptible Staphylococcus aureus (011UC4), an erythromycin-resistant Streptococcus pneumoniae (030MV2) and a β-lactamase-producing H. influenzae (350RD7). The MICs of telithromycin for these organisms, as measured by a two-fold agar dilution method,4 were 0.04, 0.15 and 0.6 mg/L, respectively.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 17:34:26 GMT 2023` Edited by `admin` on `Sat Dec 16 17:34:26 GMT 2023`
Record UNII	KI8H7H19WL
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TELITHROMYCIN

Official Name

English

TELITHROMYCIN [MART.]

Common Name

English

TELITHROMYCIN [MI]

Common Name

English

TELITHROMYCIN [USAN]

Common Name

English

LEVVIAX

Brand Name

English

Telithromycin [WHO-DD]

Common Name

English

KETEK

Brand Name

English

TELITHROMYCIN [EMA EPAR]

Common Name

English

TELITHROMYCIN [VANDF]

Common Name

English

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)-

Common Name

English

NSC-758940

Code

English

HMR-3647

Code

English

telithromycin [INN]

Common Name

English

TELITHROMYCIN [JAN]

Common Name

English

TELITHROMYCIN [ORANGE BOOK]

Common Name

English

HMR3647

Code

English

TELITHROMYCIN [HSDB]

Common Name

English

Classification Tree Code System Code

WHO-ATC

J01FA15