U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C15H28N4O4
Molecular Weight 328.4078
Optical Activity UNSPECIFIED
Defined Stereocenters 5 / 5
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PERAMIVIR ANHYDROUS

SMILES

CCC(CC)[C@@]([H])([C@@]1([H])[C@@]([H])(C[C@@]([H])([C@@]1([H])O)C(=O)O)NC(=N)N)N=C(C)O

InChI

InChIKey=XRQDFNLINLXZLB-CKIKVBCHSA-N
InChI=1S/C15H28N4O4/c1-4-8(5-2)12(18-7(3)20)11-10(19-15(16)17)6-9(13(11)21)14(22)23/h8-13,21H,4-6H2,1-3H3,(H,18,20)(H,22,23)(H4,16,17,19)/t9-,10+,11+,12-,13+/m0/s1

HIDE SMILES / InChI

Molecular Formula C15H28N4O4
Molecular Weight 328.4078
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 4 / 5
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7fdedaec-9e53-4a37-a4e4-a301c8a251b8; http://www.rxlist.com/script/main/art.asp?articlekey=185939

Peramivir is a transition-state analogue and a potent, specific influenza viral neuraminidase inhibitor. Rapivab (peramivir injection) is indicated for the treatment of acute uncomplicated influenza in patients 18 years and older who have been symptomatic for no more than 2 days. Efficacy of Rapivab is based on clinical trials in which the predominant influenza virus type was influenza A and a limited number of subjects infected with influenza B virus were enrolled. Since influenza viruses change over time emergence of resistance substitutions could decrease drug effectiveness. Other factors such as changes in viral virulence might also diminish clinical benefit of antiviral drug. Efficacy could not be established in patients with serious influenza requiring hospitalization.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: UNIPROT: O91745 (Neuraminidase)
0.0800000000000000017 nM [IC50]
0.220000000000000001 nM [EC50]
0.0449999999999999983 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
RAPIVAB

Approved Use

RAPIVAB is indicated for the treatment of acute uncomplicated influenza in patients 18 years and older who have been symptomatic for no more than 2 days.

Launch Date

1418947200000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
46800 ng/mL
600 mg single, intravenous
dose: 600 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
PERAMIVIR ANHYDROUS serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
102700 ng × h/mL
600 mg single, intravenous
dose: 600 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
PERAMIVIR ANHYDROUS serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
20 h
600 mg single, intravenous
dose: 600 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
PERAMIVIR ANHYDROUS serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
70%
600 mg single, intravenous
dose: 600 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
PERAMIVIR ANHYDROUS serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
11.4 mg/kg 1 times / day steady, intravenous
dose: 11.4 mg/kg 1 times / day
route: intravenous
experiment_type: steady
dose_type:
co-adm with
    data_source:
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
    unhealthy, 2.4-9.8 years
    population: unhealthy
    age: 2.4-9.8 years
    sex: M+F
    food_status:
    n:
    data_source:
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
    Other AEs: Leukopenia, Neutropenia...
    Other AEs:
    Leukopenia (42.9%)
    Neutropenia (14.3%)
    Hyperglycemia (42.9%)
    Hypertension (28.6%)
    AST increased (14.3%)
    ALT increased (14.3%)
    Diarrhea (14.3%)

    data_source:
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
    400 mg 2 times / day multiple, intravenous
    Highest studied dose
    dose: 400 mg 2 times / day
    route: intravenous
    experiment_type: multiple
    dose_type: Highest studied dose
    co-adm with
      data_source:
      https://pubmed.ncbi.nlm.nih.gov/27805571/
      healthy, adult
      population: healthy
      age: adult
      sex: M
      food_status:
      n:
      data_source:
      https://pubmed.ncbi.nlm.nih.gov/27805571/
      400 mg 2 times / day multiple, intravenous
      Highest studied dose
      dose: 400 mg 2 times / day
      route: intravenous
      experiment_type: multiple
      dose_type: Highest studied dose
      co-adm with
        data_source:
        https://pubmed.ncbi.nlm.nih.gov/27317305/
        healthy, adult
        population: healthy
        age: adult
        sex: M+F
        food_status:
        n:
        data_source:
        https://pubmed.ncbi.nlm.nih.gov/27317305/
        600 mg 1 times / day multiple, intramuscular
        Highest studied dose
        dose: 600 mg 1 times / day
        route: intramuscular
        experiment_type: multiple
        dose_type: Highest studied dose
        co-adm with
          data_source:
          https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
          healthy, adult
          population: healthy
          age: adult
          sex: unknown
          food_status:
          n:
          data_source:
          https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
          800 mg 1 times / day multiple, intravenous
          Highest studied dose
          dose: 800 mg 1 times / day
          route: intravenous
          experiment_type: multiple
          dose_type: Highest studied dose
          co-adm with
            data_source:
            https://pubmed.ncbi.nlm.nih.gov/27805571/
            healthy, adult
            population: healthy
            age: adult
            sex: M
            food_status:
            n:
            data_source:
            https://pubmed.ncbi.nlm.nih.gov/27805571/
            800 mg 1 times / day multiple, intravenous
            Highest studied dose
            dose: 800 mg 1 times / day
            route: intravenous
            experiment_type: multiple
            dose_type: Highest studied dose
            co-adm with
              data_source:
              https://pubmed.ncbi.nlm.nih.gov/27317305/
              healthy, adult
              population: healthy
              age: adult
              sex: M+F
              food_status:
              n:
              data_source:
              https://pubmed.ncbi.nlm.nih.gov/27317305/
              300 mg 1 times / day multiple, intravenous
              Minumum effective dose
              dose: 300 mg 1 times / day
              route: intravenous
              experiment_type: multiple
              dose_type: Minumum effective dose
              co-adm with
                data_source:
                https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                unhealthy, adult
                population: unhealthy
                age: adult
                sex: unknown
                food_status:
                n:
                data_source:
                https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                Disc. AE: Lymphadenopathy, Gingival pain...
                AEs leading to
                discontinuation/dose reduction:​
                Lymphadenopathy (<1)
                Gingival pain (<1)
                Salivary gland pain (<1)
                Rash (<1)

                data_source:
                https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                600 mg 1 times / day multiple, intravenous
                Recommended
                dose: 600 mg 1 times / day
                route: intravenous
                experiment_type: multiple
                dose_type: Recommended
                co-adm with
                  data_source:
                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                  unhealthy, adult
                  population: unhealthy
                  age: adult
                  sex: unknown
                  food_status:
                  n:
                  data_source:
                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                  Other AEs: Alanine aminotransferase, Creatine phosphokinase...
                  Other AEs:
                  Alanine aminotransferase (grade 2-4, 3%)
                  Creatine phosphokinase (grade 2-4, 4%)
                  Neutrophils (grade 2-4, 8%)

                  data_source:
                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                  600 mg 1 times / day multiple, intravenous
                  Recommended
                  dose: 600 mg 1 times / day
                  route: intravenous
                  experiment_type: multiple
                  dose_type: Recommended
                  co-adm with
                    data_source:
                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                    unhealthy, adult
                    population: unhealthy
                    age: adult
                    sex: unknown
                    food_status:
                    n:
                    data_source:
                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                    Other AEs: Serum glucose...
                    Other AEs:
                    Serum glucose (grade 2-4, 5%)

                    data_source:
                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                    600 mg 1 times / day multiple, intravenous
                    Recommended
                    dose: 600 mg 1 times / day
                    route: intravenous
                    experiment_type: multiple
                    dose_type: Recommended
                    co-adm with
                      data_source:
                      https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                      unhealthy, adult
                      population: unhealthy
                      age: adult
                      sex: unknown
                      food_status:
                      n:
                      data_source:
                      https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                      Disc. AE: Abdominal pain upper, Arthralgia...
                      AEs leading to
                      discontinuation/dose reduction:​
                      Abdominal pain upper (<1)
                      Arthralgia (<1)
                      Drug eruption (<1)
                      Eczema (<1)
                      Rash (<1)

                      data_source:
                      https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                      AEs

                      AEs

                      AESignificanceDosePopulation
                      ALT increased 14.3%
                      11.4 mg/kg 1 times / day steady, intravenous
                      dose: 11.4 mg/kg 1 times / day
                      route: intravenous
                      experiment_type: steady
                      dose_type:
                      co-adm with
                        data_source:
                        https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                        unhealthy, 2.4-9.8 years
                        population:
                        age:
                        sex:
                        food_status:
                        n:
                        data_source:
                        https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                        AST increased 14.3%
                        11.4 mg/kg 1 times / day steady, intravenous
                        dose: 11.4 mg/kg 1 times / day
                        route: intravenous
                        experiment_type: steady
                        dose_type:
                        co-adm with
                          data_source:
                          https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                          unhealthy, 2.4-9.8 years
                          population:
                          age:
                          sex:
                          food_status:
                          n:
                          data_source:
                          https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                          Diarrhea 14.3%
                          11.4 mg/kg 1 times / day steady, intravenous
                          dose: 11.4 mg/kg 1 times / day
                          route: intravenous
                          experiment_type: steady
                          dose_type:
                          co-adm with
                            data_source:
                            https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                            unhealthy, 2.4-9.8 years
                            population:
                            age:
                            sex:
                            food_status:
                            n:
                            data_source:
                            https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                            Neutropenia 14.3%
                            11.4 mg/kg 1 times / day steady, intravenous
                            dose: 11.4 mg/kg 1 times / day
                            route: intravenous
                            experiment_type: steady
                            dose_type:
                            co-adm with
                              data_source:
                              https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                              unhealthy, 2.4-9.8 years
                              population:
                              age:
                              sex:
                              food_status:
                              n:
                              data_source:
                              https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                              Hypertension 28.6%
                              11.4 mg/kg 1 times / day steady, intravenous
                              dose: 11.4 mg/kg 1 times / day
                              route: intravenous
                              experiment_type: steady
                              dose_type:
                              co-adm with
                                data_source:
                                https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                                unhealthy, 2.4-9.8 years
                                population:
                                age:
                                sex:
                                food_status:
                                n:
                                data_source:
                                https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                                Hyperglycemia 42.9%
                                11.4 mg/kg 1 times / day steady, intravenous
                                dose: 11.4 mg/kg 1 times / day
                                route: intravenous
                                experiment_type: steady
                                dose_type:
                                co-adm with
                                  data_source:
                                  https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                                  unhealthy, 2.4-9.8 years
                                  population:
                                  age:
                                  sex:
                                  food_status:
                                  n:
                                  data_source:
                                  https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                                  Leukopenia 42.9%
                                  11.4 mg/kg 1 times / day steady, intravenous
                                  dose: 11.4 mg/kg 1 times / day
                                  route: intravenous
                                  experiment_type: steady
                                  dose_type:
                                  co-adm with
                                    data_source:
                                    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                                    unhealthy, 2.4-9.8 years
                                    population:
                                    age:
                                    sex:
                                    food_status:
                                    n:
                                    data_source:
                                    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836703/
                                    Gingival pain <1%
                                    Disc. AE
                                    300 mg 1 times / day multiple, intravenous
                                    Minumum effective dose
                                    dose: 300 mg 1 times / day
                                    route: intravenous
                                    experiment_type: multiple
                                    dose_type: Minumum effective dose
                                    co-adm with
                                      data_source:
                                      https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                                      unhealthy, adult
                                      Lymphadenopathy <1%
                                      Disc. AE
                                      300 mg 1 times / day multiple, intravenous
                                      Minumum effective dose
                                      dose: 300 mg 1 times / day
                                      route: intravenous
                                      experiment_type: multiple
                                      dose_type: Minumum effective dose
                                      co-adm with
                                        data_source:
                                        https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                                        unhealthy, adult
                                        Rash <1%
                                        Disc. AE
                                        300 mg 1 times / day multiple, intravenous
                                        Minumum effective dose
                                        dose: 300 mg 1 times / day
                                        route: intravenous
                                        experiment_type: multiple
                                        dose_type: Minumum effective dose
                                        co-adm with
                                          data_source:
                                          https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                                          unhealthy, adult
                                          Salivary gland pain <1%
                                          Disc. AE
                                          300 mg 1 times / day multiple, intravenous
                                          Minumum effective dose
                                          dose: 300 mg 1 times / day
                                          route: intravenous
                                          experiment_type: multiple
                                          dose_type: Minumum effective dose
                                          co-adm with
                                            data_source:
                                            https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                                            unhealthy, adult
                                            Abdominal pain upper <1%
                                            Disc. AE
                                            600 mg 1 times / day multiple, intravenous
                                            Recommended
                                            dose: 600 mg 1 times / day
                                            route: intravenous
                                            experiment_type: multiple
                                            dose_type: Recommended
                                            co-adm with
                                              data_source:
                                              https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                                              unhealthy, adult
                                              Arthralgia <1%
                                              Disc. AE
                                              600 mg 1 times / day multiple, intravenous
                                              Recommended
                                              dose: 600 mg 1 times / day
                                              route: intravenous
                                              experiment_type: multiple
                                              dose_type: Recommended
                                              co-adm with
                                                data_source:
                                                https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                                                unhealthy, adult
                                                Drug eruption <1%
                                                Disc. AE
                                                600 mg 1 times / day multiple, intravenous
                                                Recommended
                                                dose: 600 mg 1 times / day
                                                route: intravenous
                                                experiment_type: multiple
                                                dose_type: Recommended
                                                co-adm with
                                                  data_source:
                                                  https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                                                  unhealthy, adult
                                                  Eczema <1%
                                                  Disc. AE
                                                  600 mg 1 times / day multiple, intravenous
                                                  Recommended
                                                  dose: 600 mg 1 times / day
                                                  route: intravenous
                                                  experiment_type: multiple
                                                  dose_type: Recommended
                                                  co-adm with
                                                    data_source:
                                                    https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                                                    unhealthy, adult
                                                    Rash <1%
                                                    Disc. AE
                                                    600 mg 1 times / day multiple, intravenous
                                                    Recommended
                                                    dose: 600 mg 1 times / day
                                                    route: intravenous
                                                    experiment_type: multiple
                                                    dose_type: Recommended
                                                    co-adm with
                                                      data_source:
                                                      https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206426Orig1s000ClinPharmR.pdf
                                                      unhealthy, adult
                                                      Alanine aminotransferase grade 2-4,3%
                                                      600 mg 1 times / day multiple, intravenous
                                                      Recommended
                                                      dose: 600 mg 1 times / day
                                                      route: intravenous
                                                      experiment_type: multiple
                                                      dose_type: Recommended
                                                      co-adm with
                                                        data_source:
                                                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                                                        unhealthy, adult
                                                        population:
                                                        age:
                                                        sex:
                                                        food_status:
                                                        n:
                                                        data_source:
                                                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                                                        Creatine phosphokinase grade 2-4,4%
                                                        600 mg 1 times / day multiple, intravenous
                                                        Recommended
                                                        dose: 600 mg 1 times / day
                                                        route: intravenous
                                                        experiment_type: multiple
                                                        dose_type: Recommended
                                                        co-adm with
                                                          data_source:
                                                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                                                          unhealthy, adult
                                                          population:
                                                          age:
                                                          sex:
                                                          food_status:
                                                          n:
                                                          data_source:
                                                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                                                          Serum glucose grade 2-4,5%
                                                          600 mg 1 times / day multiple, intravenous
                                                          Recommended
                                                          dose: 600 mg 1 times / day
                                                          route: intravenous
                                                          experiment_type: multiple
                                                          dose_type: Recommended
                                                          co-adm with
                                                            data_source:
                                                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                                                            unhealthy, adult
                                                            population:
                                                            age:
                                                            sex:
                                                            food_status:
                                                            n:
                                                            data_source:
                                                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                                                            Neutrophils grade 2-4,8%
                                                            600 mg 1 times / day multiple, intravenous
                                                            Recommended
                                                            dose: 600 mg 1 times / day
                                                            route: intravenous
                                                            experiment_type: multiple
                                                            dose_type: Recommended
                                                            co-adm with
                                                              data_source:
                                                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                                                              unhealthy, adult
                                                              population:
                                                              age:
                                                              sex:
                                                              food_status:
                                                              n:
                                                              data_source:
                                                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206426lbl.pdf
                                                              PubMed

                                                              PubMed

                                                              TitleDatePubMed
                                                              BCX-1812 (RWJ-270201): discovery of a novel, highly potent, orally active, and selective influenza neuraminidase inhibitor through structure-based drug design.
                                                              2000 Sep 21
                                                              Comparison of the anti-influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir.
                                                              2001 Apr
                                                              Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants.
                                                              2001 Dec
                                                              Characterization of an influenza A (H3N2) virus resistant to the cyclopentane neuraminidase inhibitor RWJ-270201.
                                                              2001 Dec
                                                              Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity.
                                                              2001 Dec 6
                                                              Primary immune system effects of the orally administered cyclopentane neuraminidase inhibitor RWJ-270201 in influenza virus-infected mice.
                                                              2001 Jun
                                                              In vivo influenza virus-inhibitory effects of the cyclopentane neuraminidase inhibitor RJW-270201.
                                                              2001 Mar
                                                              Cyclopentane neuraminidase inhibitors with potent in vitro anti-influenza virus activities.
                                                              2001 Mar
                                                              Comparison of efficacies of RWJ-270201, zanamivir, and oseltamivir against H5N1, H9N2, and other avian influenza viruses.
                                                              2001 Oct
                                                              Influence of virus strain, challenge dose, and time of therapy initiation on the in vivo influenza inhibitory effects of RWJ-270201.
                                                              2001 Sep
                                                              In vitro characterization of A-315675, a highly potent inhibitor of A and B strain influenza virus neuraminidases and influenza virus replication.
                                                              2002 Apr
                                                              Peramivir (BCX-1812, RWJ-270201): potential new therapy for influenza.
                                                              2002 Jun
                                                              Combination treatment of influenza A virus infections in cell culture and in mice with the cyclopentane neuraminidase inhibitor RWJ-270201 and ribavirin.
                                                              2002 May
                                                              Structural studies of the resistance of influenza virus neuramindase to inhibitors.
                                                              2002 May 23
                                                              Comparison of colorimetric, fluorometric, and visual methods for determining anti-influenza (H1N1 and H3N2) virus activities and toxicities of compounds.
                                                              2002 Oct
                                                              Inhibition of influenza virus infections in immunosuppressed mice with orally administered peramivir (BCX-1812).
                                                              2003 Sep
                                                              A QSAR study on influenza neuraminidase inhibitors.
                                                              2006 Feb 15
                                                              Patents

                                                              Sample Use Guides

                                                              The recommended dose of RAPIVAB in adult patients 18 years of age or older with acute uncomplicated influenza is a single 600 mg dose, administered via intravenous infusion for 15 to 30 minutes. The dose should be reduced for patients with baseline creatinine clearance below 50 mL/min to 200 mg dose (at 30-49 mL/min creatinine clearance), and 100 mg dose (at 10-29 mL/min creatinine clearance).
                                                              Route of Administration: Intravenous
                                                              The concentrations of peramivir required for inhibition of influenza virus in cell culture varied with the virus strain tested. The effect of antiviral compounds on the replication of influenza viruses in MDCK cells was determined by flow cytometric analysis of virus-infected cells. The mean 50% effective concentrations (EC50 values) of peramivir were in the range of 0.045-0.071 nM), 0.065-0.07 nM and 0.215-33.58 nM for influenza A/H1N1 virus, A/H3N2 virus, and B virus strains, respectively.
                                                              Substance Class Chemical
                                                              Created
                                                              by admin
                                                              on Fri Jun 25 23:58:14 UTC 2021
                                                              Edited
                                                              by admin
                                                              on Fri Jun 25 23:58:14 UTC 2021
                                                              Record UNII
                                                              9ZS94HQO3B
                                                              Record Status Validated (UNII)
                                                              Record Version
                                                              • Download
                                                              Name Type Language
                                                              PERAMIVIR ANHYDROUS
                                                              Common Name English
                                                              RWJ-270201
                                                              Code English
                                                              (1S,2S,3R,4R)-3-((1S)-1-ACETYLAMINO-2-ETHYLBUTYL)-4-((AMINOIMINOMETHYL)AMINO)-2-HYDROXYCYCLOPENTANECARBOXYLIC ACID
                                                              Systematic Name English
                                                              PERAMIVIR [INN]
                                                              Common Name English
                                                              PERAMIVIR [MI]
                                                              Common Name English
                                                              Code System Code Type Description
                                                              EVMPD
                                                              SUB32136
                                                              Created by admin on Fri Jun 25 23:58:14 UTC 2021 , Edited by admin on Fri Jun 25 23:58:14 UTC 2021
                                                              PRIMARY
                                                              PUBCHEM
                                                              154234
                                                              Created by admin on Fri Jun 25 23:58:14 UTC 2021 , Edited by admin on Fri Jun 25 23:58:14 UTC 2021
                                                              PRIMARY
                                                              CAS
                                                              330600-85-6
                                                              Created by admin on Fri Jun 25 23:58:14 UTC 2021 , Edited by admin on Fri Jun 25 23:58:14 UTC 2021
                                                              PRIMARY
                                                              MERCK INDEX
                                                              M8534
                                                              Created by admin on Fri Jun 25 23:58:14 UTC 2021 , Edited by admin on Fri Jun 25 23:58:14 UTC 2021
                                                              PRIMARY Merck Index
                                                              INN
                                                              8184
                                                              Created by admin on Fri Jun 25 23:58:14 UTC 2021 , Edited by admin on Fri Jun 25 23:58:14 UTC 2021
                                                              PRIMARY
                                                              WIKIPEDIA
                                                              PERAMIVIR
                                                              Created by admin on Fri Jun 25 23:58:14 UTC 2021 , Edited by admin on Fri Jun 25 23:58:14 UTC 2021
                                                              PRIMARY
                                                              FDA UNII
                                                              9ZS94HQO3B
                                                              Created by admin on Fri Jun 25 23:58:14 UTC 2021 , Edited by admin on Fri Jun 25 23:58:14 UTC 2021
                                                              PRIMARY
                                                              NCI_THESAURUS
                                                              C175841
                                                              Created by admin on Fri Jun 25 23:58:14 UTC 2021 , Edited by admin on Fri Jun 25 23:58:14 UTC 2021
                                                              PRIMARY
                                                              RXCUI
                                                              1598096
                                                              Created by admin on Fri Jun 25 23:58:14 UTC 2021 , Edited by admin on Fri Jun 25 23:58:14 UTC 2021
                                                              PRIMARY RxNorm
                                                              Related Record Type Details
                                                              EXCRETED UNCHANGED
                                                              URINE
                                                              BINDER->LIGAND
                                                              In vitro, human plasma protein binding was determined to be low (<18%) across a range of peramivir concentrations (10-1000 ng/mL) with no partitioning into red blood cells (Study DM99362).
                                                              BINDING
                                                              SALT/SOLVATE -> PARENT
                                                              Related Record Type Details
                                                              ACTIVE MOIETY
                                                              Name Property Type Amount Referenced Substance Defining Parameters References
                                                              Biological Half-life PHARMACOKINETIC SINGLE DOSE

                                                              INTRAVENOUS ADMINISTRATION

                                                              Volume of Distribution PHARMACOKINETIC
                                                              Tmax PHARMACOKINETIC INTRAVENOUS ADMINISTRATION

                                                              SINGLE DOSE