Details of the Drug

General Information of Drug (ID: DM50ILT)

Drug Name
Fostemsavir
Synonyms
BMS-216; BMS-248; BMS-378806; BMS-626529; BMS-705; BMS-806; BMS-806 series; BMS-853; HIV-1 attachment inhibitors, BMS; HIV-1 entry inhibitors, BMS; BMS-488043 follow-on compounds, BMS; HIV-1 attachment inhibitors, Bristol-Myers Squibb
Indication
Disease Entry ICD 11 Status REF
Human immunodeficiency virus infection 1C62 Approved [1]
Affected Organisms
HIV-1
ATC Code
J05AX29: Fostemsavir
J05AX: Other antivirals
J05A: DIRECT ACTING ANTIVIRALS
J05: ANTIVIRALS FOR SYSTEMIC USE
J: ANTIINFECTIVES FOR SYSTEMIC USE
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 2 Molecular Weight (mw) 583.5
Logarithm of the Partition Coefficient (xlogp) -0.1
Rotatable Bond Count (rotbonds) 8
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 11
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 12.9 mcgh/L [2]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 1770 mcg/L [2]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 2 h [2]
Bioavailability
The bioavailability of drug is 26.9% [2]
Clearance
The clearance of drug is 17.9 L/h [3]
Elimination
Approximately 51% of a given dose is excreted in the urine, with <2% comprising unchanged parent drug, and 33% is excreted in the feces, of which 1.1% is unchanged parent drug [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 11 hours [3]
Metabolism
The drug is metabolized via the alkaline phosphatase present at the brush border membrane of the intestinal lumen [2]
Vd
The volume of distribution (Vd) of drug is 29.5 L [3]
Chemical Identifiers
Formula
C25H26N7O8P
IUPAC Name
[3-[2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl]-4-methoxy-7-(3-methyl-1,2,4-triazol-1-yl)pyrrolo[2,3-c]pyridin-1-yl]methyl dihydrogen phosphate
Canonical SMILES
CC1=NN(C=N1)C2=NC=C(C3=C2N(C=C3C(=O)C(=O)N4CCN(CC4)C(=O)C5=CC=CC=C5)COP(=O)(O)O)OC
InChI
InChI=1S/C25H26N7O8P/c1-16-27-14-32(28-16)23-21-20(19(39-2)12-26-23)18(13-31(21)15-40-41(36,37)38)22(33)25(35)30-10-8-29(9-11-30)24(34)17-6-4-3-5-7-17/h3-7,12-14H,8-11,15H2,1-2H3,(H2,36,37,38)
InChIKey
SWMDAPWAQQTBOG-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
11319217
CAS Number
864953-29-7
UNII
97IQ273H4L
DrugBank ID
DB11796
TTD ID
D00ZCT
ACDINA ID
D01108
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Human immunodeficiency virus Envelope glycoprotein gp120 (HIV gp120) TTBYP1X ENV_HV1H2 Inhibitor [1]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Fostemsavir
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
MK-1439 DM215WE Minor Increased metabolism of Fostemsavir caused by MK-1439 mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [4]
Coadministration of a Drug Treating the Disease Different from Fostemsavir (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Fostemsavir and Ivosidenib. Acute myeloid leukaemia [2A60] [5]
Gilteritinib DMTI0ZO Moderate Increased risk of prolong QT interval by the combination of Fostemsavir and Gilteritinib. Acute myeloid leukaemia [2A60] [6]
Levalbuterol DM5YBO1 Moderate Increased risk of prolong QT interval by the combination of Fostemsavir and Levalbuterol. Asthma [CA23] [7]
ABT-492 DMJFD2I Moderate Decreased clearance of Fostemsavir due to the transporter inhibition by ABT-492. Bacterial infection [1A00-1C4Z] [4]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Fostemsavir caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [4]
Pexidartinib DMS2J0Z Minor Increased metabolism of Fostemsavir caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [8]
Alpelisib DMEXMYK Moderate Decreased clearance of Fostemsavir due to the transporter inhibition by Alpelisib. Breast cancer [2C60-2C6Y] [4]
PF-04449913 DMSB068 Moderate Increased risk of prolong QT interval by the combination of Fostemsavir and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [9]
Revefenacin DMMP5SI Moderate Decreased clearance of Fostemsavir due to the transporter inhibition by Revefenacin. Chronic obstructive pulmonary disease [CA22] [10]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Fostemsavir and Osilodrostat. Cushing syndrome [5A70] [11]
Eslicarbazepine DMZREFQ Minor Increased metabolism of Fostemsavir caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [4]
Tazemetostat DMWP1BH Minor Increased metabolism of Fostemsavir caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [8]
Brigatinib DM7W94S Minor Increased metabolism of Fostemsavir caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [4]
PF-06463922 DMKM7EW Minor Increased metabolism of Fostemsavir caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [4]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Fostemsavir and Selpercatinib. Lung cancer [2C25] [12]
Rimegepant DMHOAUG Moderate Decreased clearance of Fostemsavir due to the transporter inhibition by Rimegepant. Migraine [8A80] [13]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Fostemsavir and Siponimod. Multiple sclerosis [8A40] [14]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Fostemsavir and Ozanimod. Multiple sclerosis [8A40] [15]
Entrectinib DMMPTLH Moderate Increased risk of prolong QT interval by the combination of Fostemsavir and Entrectinib. Non-small cell lung cancer [2C25] [14]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Fostemsavir and Rucaparib. Ovarian cancer [2C73] [4]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Fostemsavir and Triclabendazole. Parasitic worm infestation [1F90] [4]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Fostemsavir and Lefamulin. Pneumonia [CA40] [5]
Relugolix DMK7IWL Moderate Increased risk of prolong QT interval by the combination of Fostemsavir and Relugolix. Prostate cancer [2C82] [11]
Telotristat ethyl DMDIYFZ Minor Increased metabolism of Fostemsavir caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [8]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Fostemsavir due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [16]
Elagolix DMB2C0E Minor Increased metabolism of Fostemsavir caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [8]
⏷ Show the Full List of 26 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Hydroxypropyl cellulose E00632 Not Available Binding agent; Coating agent; Emulsifying agent; Film/Membrane-forming agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
Hypromellose E00634 Not Available Coating agent
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 4000 E00654 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyvinyl alcohol E00666 Not Available Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Haematite red E00236 14833 Colorant
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
⏷ Show the Full List of 10 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Fostemsavir 600mg Extended-Release tablet 600mg Extended-Release Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2020
2 Yu HZ, Han SF, Li P, Zhu CL, Zhang XX, Gan L, Gan Y: An examination of the potential effect of lipids on the first-pass metabolism of the lipophilic drug anethol trithione. J Pharm Sci. 2011 Nov;100(11):5048-58. doi: 10.1002/jps.22702. Epub 2011 Jul 15.
3 FDA Approved Drug Products: Rukobia (fostemsavir) extended-release tablets
4 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
5 Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ.
6 Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL.
7 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
8 Product Information. Diabinese (chlorpropamide). Pfizer US Pharmaceuticals, New York, NY.
9 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
10 Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI.
11 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
12 Product Information. Retevmo (selpercatinib). Lilly, Eli and Company, Indianapolis, IN.
13 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
14 Cerner Multum, Inc. "Australian Product Information.".
15 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
16 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".