Identification

Name
Oritavancin
Accession Number
DB04911
Description

Oritavancin is a glycopeptide antibiotic used for the treatment of skin infections. It was developed by The Medicines Company (acquired by Novartis).10 Oritavancin was initially approved by the FDA in 2014 and formulated to combat resistant Staphylococcus, Streptococcus, and other gram-positive bacteria that cause skin infections. It boasts the option of single-dose administration that has been proven as non-inferior to a full course of vancomycin therapy.8,9

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 1793.101
Monoisotopic: 1790.564106447
Chemical Formula
C86H97Cl3N10O26
Synonyms
  • Chlorobiphenyl-chloroeremomycin
  • Oritavancin
External IDs
  • LY-333328
  • LY333328

Pharmacology

Indication

Oritavancin is indicated for the treatment of adult patients with acute bacterial skin and skin structure (including subcutaneous) infection. It is used for confirmed/suspected infections with designated and susceptible gram-positive organisms.9

As antimicrobial susceptibility patterns are geographically distinct, local antibiograms should be consulted to ensure adequate coverage of relevant pathogens prior to use.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Oritavancin interferes with bacterial cell wall synthesis and integrity, treating susceptible skin and subcutaneous tissue infections with gram-positive bacteria.3,9 This drug is known to artifically increase INR and aPTT, interfering with coagulation testing. Cases of infusion reactions have also been reported.9

Mechanism of action

The cell wall is vital for the survival and replication of bacteria, making it a primary target for antibiotic therapy.4 Oritavancin works against susceptible gram-positive organisms via three separate mechanisms. Firstly, it binds to the stem peptide of peptidoglycan precursors, inhibiting transglycosylation (polymerization). This process normally occurs during cell wall synthesis. Secondly, oritavancin inhibits crosslinking during bacterial cell wall biosynthesis via binding to cell wall pentaglycyl peptide bridging segments. Finally, this drug also acts by disrupting the bacterial cell membrane, interfering with its integrity, which eventually leads to cell death by various mechanisms.5,6,9

TargetActionsOrganism
APeptidoglycan precursors
binder
ABacterial cell wall peptide bridging segments
inhibitor
Staphylococcus aureus
APentaglycyl bridging segment
disruptor
Staphylococcus aureus
Absorption

Pharmacokinetic analysis of oritavancin revealed a Cmax of 138 and μg/mL and an AUC0-∞ of 2800 μg•h/mL.9 The AUC0-t in a study of healthy volunteers after an 800 mg dose 1,1111 μg•h/mL.1 was also be Another pharmacokinetic study reported a Cmax of 4.7-7.6 micrograms/mL, generally achieved within 24 hours of administration.2

Volume of distribution

The volume of distribution of oritavancin is estimated at 87.6 L, suggesting extensive tissue distribution.9

Protein binding

Oritavancin is about 85% bound to plasma proteins.9

Metabolism

In vitro studies on human hepatocytes suggest that oritavancin is not metabolized, and is excreted unchanged.7,9

Route of elimination

Oritavancin is excreted as unchanged drug in both the urine and feces. Less than 5% has been recovered in the urine, and 1% has been recovered in the feces.2,9

Half-life

The average terminal half-life of oritavancin is about 245 hours.9 A pharmacokinetic study revealed a terminal half-life ranging from 135.8-273.8 hours.2

Clearance

The clearance of oritavancin is approximately 0.445 L/h.9 One study revealed a renal clearance of 0.457 mL/min.2

Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

The LD50 of oritavancin in rats is >500m mg/kg.12 Prescribing information indicates no experience with overdose during the clinical program for oritavancin, however, an overdose is likely to result in an increased risk of adverse effects, such as headache, nausea vomiting, and diarrhea. This drug is not dialyzable, and in the case of an overdose, supportive measures should be undertaken.9

Affected organisms
  • Gram-positive Bacteria
  • Streptococcus pyogenes
  • Streptococcus pneumoniae
  • Staphylococcus aureus
  • Enterococcus faecalis
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbirateroneThe metabolism of Abiraterone can be increased when combined with Oritavancin.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Oritavancin.
AcebutololThe metabolism of Acebutolol can be decreased when combined with Oritavancin.
AcenocoumarolThe risk or severity of bleeding can be increased when Oritavancin is combined with Acenocoumarol.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Oritavancin.
AcetohexamideThe metabolism of Acetohexamide can be decreased when combined with Oritavancin.
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be decreased when combined with Oritavancin.
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Oritavancin.
AlectinibThe metabolism of Alectinib can be increased when combined with Oritavancin.
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Oritavancin.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
No interactions found.

Products

Product Ingredients
IngredientUNIICASInChI Key
Oritavancin diphosphateVL1P93MKZN192564-14-0PWTROOMOPLCZHB-BHYQHFGMSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
OrbactivInjection, powder, lyophilized, for solution400 mg/1IntravenousThe Medicines Company2014-09-012021-06-30US flag
OrbactivInjection, powder, lyophilized, for solution400 mg/1IntravenousMelinta Therapeutics, Inc.2014-09-01Not applicableUS flag
OrbactivInjection, powder, lyophilized, for solution400 mg/1IntravenousThe Medicines Company2014-09-012014-08-12US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
J01XA05 — Oritavancin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Oligopeptides
Alternative Parents
Cyclic peptides / Aminoglycosides / Phenolic glycosides / Leucine and derivatives / Chlorinated biphenyls / N-acyl-alpha amino acids and derivatives / Alpha amino acid amides / Diarylethers / Disaccharides / O-glycosyl compounds
show 29 more
Substituents
1,2-aminoalcohol / 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / Acetal / Alcohol / Alpha-amino acid amide / Alpha-amino acid or derivatives / Alpha-oligopeptide / Amine / Amino acid
show 55 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
disaccharide derivative, glycopeptide (CHEBI:82699)

Chemical Identifiers

UNII
PUG62FRZ2E
CAS number
171099-57-3
InChI Key
VHFGEBVPHAGQPI-LXKZPTCJSA-N
InChI
InChI=1S/C86H97Cl3N10O26/c1-35(2)22-51(92-7)77(110)98-67-69(105)42-15-20-55(49(88)24-42)120-57-26-44-27-58(73(57)125-84-74(71(107)70(106)59(34-100)122-84)124-62-32-86(6,76(109)37(4)119-62)93-33-38-8-10-39(11-9-38)40-12-17-45(87)18-13-40)121-56-21-16-43(25-50(56)89)72(123-61-31-85(5,91)75(108)36(3)118-61)68-82(115)97-66(83(116)117)48-28-46(101)29-54(103)63(48)47-23-41(14-19-53(47)102)64(79(112)99-68)96-80(113)65(44)95-78(111)52(30-60(90)104)94-81(67)114/h8-21,23-29,35-37,51-52,59,61-62,64-72,74-76,84,92-93,100-103,105-109H,22,30-34,91H2,1-7H3,(H2,90,104)(H,94,114)(H,95,111)(H,96,113)(H,97,115)(H,98,110)(H,99,112)(H,116,117)/t36-,37-,51+,52-,59+,61-,62-,64+,65+,66-,67+,68-,69+,70+,71-,72+,74+,75-,76-,84-,85-,86-/m0/s1
IUPAC Name
(1S,2R,18R,19R,22S,25R,28R,40S)-2-{[(2R,4S,5R,6S)-4-amino-5-hydroxy-4,6-dimethyloxan-2-yl]oxy}-22-(carbamoylmethyl)-5,47-dichloro-48-{[(2S,3R,4S,5S,6R)-3-{[(2S,4S,5R,6S)-4-[({4'-chloro-[1,1'-biphenyl]-4-yl}methyl)amino]-5-hydroxy-4,6-dimethyloxan-2-yl]oxy}-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-18,32,35,37-tetrahydroxy-19-[(2R)-4-methyl-2-(methylamino)pentanamido]-20,23,26,42,44-pentaoxo-7,13-dioxa-21,24,27,41,43-pentaazaoctacyclo[26.14.2.2^{3,6}.2^{14,17}.1^{8,12}.1^{29,33}.0^{10,25}.0^{34,39}]pentaconta-3,5,8,10,12(48),14,16,29(45),30,32,34,36,38,46,49-pentadecaene-40-carboxylic acid
SMILES
CN[[email protected]](CC(C)C)C(=O)N[[email protected]@H]1[[email protected]](O)C2=CC=C(OC3=C(O[[email protected]@H]4O[[email protected]](CO)[[email protected]@H](O)[[email protected]](O)[[email protected]]4O[[email protected]]4C[[email protected]](C)(NCC5=CC=C(C=C5)C5=CC=C(Cl)C=C5)[[email protected]@H](O)[[email protected]](C)O4)C4=CC(=C3)[[email protected]@H](NC(=O)[[email protected]](CC(N)=O)NC1=O)C(=O)N[[email protected]@H]1C3=CC(=C(O)C=C3)C3=C(O)C=C(O)C=C3[[email protected]](NC(=O)[[email protected]@H](NC1=O)[[email protected]](O[[email protected]]1C[[email protected]](C)(N)[[email protected]@H](O)[[email protected]](C)O1)C1=CC(Cl)=C(O4)C=C1)C(O)=O)C(Cl)=C2

References

Synthesis Reference

Adel Rafai Far, Gopal Krishna, Min Ding, Sanjay R, Chemburkar Carl M, Knable James, J. PETZEL, Julie J Pruyne, Douglas M. Reamer.2015. High purity oritavancin and method of producing same.Patent WO2016011245A1

General References
  1. Fetterly GJ, Ong CM, Bhavnani SM, Loutit JS, Porter SB, Morello LG, Ambrose PG, Nicolau DP: Pharmacokinetics of oritavancin in plasma and skin blister fluid following administration of a 200-milligram dose for 3 days or a single 800-milligram dose. Antimicrob Agents Chemother. 2005 Jan;49(1):148-52. [PubMed:15616289]
  2. Bhavnani SM, Owen JS, Loutit JS, Porter SB, Ambrose PG: Pharmacokinetics, safety, and tolerability of ascending single intravenous doses of oritavancin administered to healthy human subjects. Diagn Microbiol Infect Dis. 2004 Oct;50(2):95-102. [PubMed:15474317]
  3. Kmeid J, Kanafani ZA: Oritavancin for the treatment of acute bacterial skin and skin structure infections: an evidence-based review. Core Evid. 2015 Feb 11;10:39-47. doi: 10.2147/CE.S51284. eCollection 2015. [PubMed:25709561]
  4. Schuerholz T, Domming S, Hornef M, Dupont A, Kowalski I, Kaconis Y, Heinbockel L, Andra J, Garidel P, Gutsmann T, David S, Sanchez-Gomez S, Martinez de Tejada G, Brandenburg K: Bacterial cell wall compounds as promising targets of antimicrobial agents II. Immunological and clinical aspects. Curr Drug Targets. 2012 Aug;13(9):1131-7. doi: 10.2174/138945012802002438. [PubMed:22664073]
  5. Kim SJ, Cegelski L, Stueber D, Singh M, Dietrich E, Tanaka KS, Parr TR Jr, Far AR, Schaefer J: Oritavancin exhibits dual mode of action to inhibit cell-wall biosynthesis in Staphylococcus aureus. J Mol Biol. 2008 Mar 14;377(1):281-93. doi: 10.1016/j.jmb.2008.01.031. Epub 2008 Jan 17. [PubMed:18258256]
  6. Zhanel GG, Schweizer F, Karlowsky JA: Oritavancin: mechanism of action. Clin Infect Dis. 2012 Apr;54 Suppl 3:S214-9. doi: 10.1093/cid/cir920. [PubMed:22431851]
  7. Cada DJ, Baker DE: Oritavancin diphosphate. Hosp Pharm. 2014 Dec;49(11):1049-60. doi: 10.1310/hjp4911-1049. [PubMed:25673895]
  8. Corey GR, Kabler H, Mehra P, Gupta S, Overcash JS, Porwal A, Giordano P, Lucasti C, Perez A, Good S, Jiang H, Moeck G, O'Riordan W: Single-dose oritavancin in the treatment of acute bacterial skin infections. N Engl J Med. 2014 Jun 5;370(23):2180-90. doi: 10.1056/NEJMoa1310422. [PubMed:24897083]
  9. FDA Approved Drug Products: Orbactiv (oritavancin) for intravenous injection [Link]
  10. Novartis successfully completes acquisition of The Medicines Company, adding a potentially first-in-class, investigational cholesterol-lowering therapy inclisiran [Link]
  11. DailyMed: Orbactiv (oritavancin) powder for injection [Link]
  12. Mckesson: Oritavancin diphosphate MSDS [Link]
  13. Orbactiv website [Link]
KEGG Compound
C12034
PubChem Compound
16136912
PubChem Substance
175426900
ChemSpider
17286443
RxNav
1547611
ChEBI
82699
ChEMBL
CHEMBL1688530
Wikipedia
Oritavancin
FDA label
Download (527 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedOtherSkin Diseases, Bacterial1
4CompletedTreatmentAcute acute bacterial skin and skin structure infections1
4RecruitingTreatmentStaphylococcus Aureus Bacteraemia / Staphylococcus Aureus Endocarditis1
3CompletedTreatmentAbscesses / Cellulitis / Systemic Inflammation / Wound Infections2
2CompletedTreatmentAbscesses / Cellulitis / Staphylococcal Skin Infections / Streptococcal Infections / Wounds and Injuries1
1CompletedNot AvailableHealthy Volunteers3
1CompletedBasic ScienceAcute acute bacterial skin and skin structure infections1
1CompletedTreatmentHealthy Volunteers3
1RecruitingTreatmentGram Positive Bacterial Infections / Infections, Gram-Positive Bacterial1
Not AvailableCompletedNot AvailableInfections, Gram-Positive Bacterial1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, for solutionIntravenous400 MG
Injection, powder, lyophilized, for solutionIntravenous400 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8420592No2013-04-162029-08-29US flag
US5840684No1998-11-242016-11-24US flag
US5998581No1999-12-072017-11-12US flag
US9649352No2017-05-162035-07-16US flag
US9682061No2017-06-202030-04-26US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
boiling point (°C)810.3http://www.demechem.com/English/productshow.asp?id=49
water solubility10 mg/mLhttps://www.sigmaaldrich.com/catalog/product/sigma/sml1586?lang=fr®ion=CA
logP4.1PMID: 18375379
pKa2.93±0.7https://www.chemicalbook.com/ChemicalProductProperty_EN_CB92451283.htm
Predicted Properties
PropertyValueSource
Water Solubility0.0588 mg/mLALOGPS
logP1.92ALOGPS
logP0.2ChemAxon
logS-4.5ALOGPS
pKa (Strongest Acidic)2.98ChemAxon
pKa (Strongest Basic)9.96ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count27ChemAxon
Hydrogen Donor Count20ChemAxon
Polar Surface Area560.98 Å2ChemAxon
Rotatable Bond Count19ChemAxon
Refractivity441.59 m3·mol-1ChemAxon
Polarizability178.55 Å3ChemAxon
Number of Rings13ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption-0.6087
Blood Brain Barrier-0.9905
Caco-2 permeable-0.7039
P-glycoprotein substrateSubstrate0.9233
P-glycoprotein inhibitor INon-inhibitor0.8502
P-glycoprotein inhibitor IINon-inhibitor0.9262
Renal organic cation transporterNon-inhibitor0.9503
CYP450 2C9 substrateNon-substrate0.8721
CYP450 2D6 substrateNon-substrate0.8153
CYP450 3A4 substrateSubstrate0.6616
CYP450 1A2 substrateNon-inhibitor0.881
CYP450 2C9 inhibitorNon-inhibitor0.8283
CYP450 2D6 inhibitorNon-inhibitor0.8541
CYP450 2C19 inhibitorNon-inhibitor0.8122
CYP450 3A4 inhibitorNon-inhibitor0.6912
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7622
Ames testNon AMES toxic0.6154
CarcinogenicityNon-carcinogens0.8151
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6222 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9983
hERG inhibition (predictor II)Non-inhibitor0.5464
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

1. Peptidoglycan precursors
Kind
Group
Organism
Not Available
Pharmacological action
Yes
Actions
Binder
References
  1. Munch D, Engels I, Muller A, Reder-Christ K, Falkenstein-Paul H, Bierbaum G, Grein F, Bendas G, Sahl HG, Schneider T: Structural variations of the cell wall precursor lipid II and their influence on binding and activity of the lipoglycopeptide antibiotic oritavancin. Antimicrob Agents Chemother. 2015 Feb;59(2):772-81. doi: 10.1128/AAC.02663-14. Epub 2014 Nov 17. [PubMed:25403671]
  2. Kim SJ, Cegelski L, Stueber D, Singh M, Dietrich E, Tanaka KS, Parr TR Jr, Far AR, Schaefer J: Oritavancin exhibits dual mode of action to inhibit cell-wall biosynthesis in Staphylococcus aureus. J Mol Biol. 2008 Mar 14;377(1):281-93. doi: 10.1016/j.jmb.2008.01.031. Epub 2008 Jan 17. [PubMed:18258256]
  3. FDA Approved Drug Products: Orbactiv (oritavancin) for intravenous injection [Link]
2. Bacterial cell wall peptide bridging segments
Kind
Group
Organism
Staphylococcus aureus
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
Staphylococcus aureus has been selected as a representative organism, however this drug also targets other susceptible gram positive organisms.
References
  1. Kim SJ, Cegelski L, Stueber D, Singh M, Dietrich E, Tanaka KS, Parr TR Jr, Far AR, Schaefer J: Oritavancin exhibits dual mode of action to inhibit cell-wall biosynthesis in Staphylococcus aureus. J Mol Biol. 2008 Mar 14;377(1):281-93. doi: 10.1016/j.jmb.2008.01.031. Epub 2008 Jan 17. [PubMed:18258256]
  2. Zhanel GG, Schweizer F, Karlowsky JA: Oritavancin: mechanism of action. Clin Infect Dis. 2012 Apr;54 Suppl 3:S214-9. doi: 10.1093/cid/cir920. [PubMed:22431851]
  3. FDA Approved Drug Products: Orbactiv (oritavancin) for intravenous injection [Link]
3. Pentaglycyl bridging segment
Kind
Group
Organism
Staphylococcus aureus
Pharmacological action
Yes
Actions
Disruptor
Curator comments
Staphylococcus aureus has been selected as a representative organism, however this drug also targets other susceptible gram positive organisms.
References
  1. Kim SJ, Cegelski L, Stueber D, Singh M, Dietrich E, Tanaka KS, Parr TR Jr, Far AR, Schaefer J: Oritavancin exhibits dual mode of action to inhibit cell-wall biosynthesis in Staphylococcus aureus. J Mol Biol. 2008 Mar 14;377(1):281-93. doi: 10.1016/j.jmb.2008.01.031. Epub 2008 Jan 17. [PubMed:18258256]
  2. Zhanel GG, Schweizer F, Karlowsky JA: Oritavancin: mechanism of action. Clin Infect Dis. 2012 Apr;54 Suppl 3:S214-9. doi: 10.1093/cid/cir920. [PubMed:22431851]
  3. FDA Approved Drug Products: Orbactiv (oritavancin) for intravenous injection [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Vitamin d3 25-hydroxylase activity
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 performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. FDA Approved Drug Products: Orbactiv (oritavancin) for intravenous injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
Curator comments
While CYP2D6 is generally not an inducible enzyme, the FDA Label states that oritavancin may induce CYP2D6 based on general activity of oritavancin on other CYP enzymes. There is not enough evidence that such modulation of the enzyme will lead to clinically significant drug-drug interactions.
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Cada DJ, Baker DE: Oritavancin diphosphate. Hosp Pharm. 2014 Dec;49(11):1049-60. doi: 10.1310/hjp4911-1049. [PubMed:25673895]
  2. Brade KD, Rybak JM, Rybak MJ: Oritavancin: A New Lipoglycopeptide Antibiotic in the Treatment of Gram-Positive Infections. Infect Dis Ther. 2016 Mar;5(1):1-15. doi: 10.1007/s40121-016-0103-4. Epub 2016 Feb 1. [PubMed:26831328]
  3. FDA Approved Drug Products: Orbactiv (oritavancin) for intravenous injection [Link]
  4. EMA Assessment Report: Orbactiv [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Rosenthal S, Decano AG, Bandali A, Lai D, Malat GE, Bias TE: Oritavancin (Orbactiv): A New-Generation Lipoglycopeptide for the Treatment Of Acute Bacterial Skin and Skin Structure Infections. P T. 2018 Mar;43(3):143-179. [PubMed:29491695]
  2. Cada DJ, Baker DE: Oritavancin diphosphate. Hosp Pharm. 2014 Dec;49(11):1049-60. doi: 10.1310/hjp4911-1049. [PubMed:25673895]
  3. Oritavancin FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Brade KD, Rybak JM, Rybak MJ: Oritavancin: A New Lipoglycopeptide Antibiotic in the Treatment of Gram-Positive Infections. Infect Dis Ther. 2016 Mar;5(1):1-15. doi: 10.1007/s40121-016-0103-4. Epub 2016 Feb 1. [PubMed:26831328]
  2. Cada DJ, Baker DE: Oritavancin diphosphate. Hosp Pharm. 2014 Dec;49(11):1049-60. doi: 10.1310/hjp4911-1049. [PubMed:25673895]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. McKay GA, Beaulieu S, Sarmiento I, Arhin FF, Parr TR Jr, Moeck G: Impact of human serum albumin on oritavancin in vitro activity against enterococci. Antimicrob Agents Chemother. 2009 Jun;53(6):2687-9. doi: 10.1128/AAC.00197-09. Epub 2009 Apr 6. [PubMed:19349514]

Drug created on October 21, 2007 16:23 / Updated on June 12, 2020 11:41

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