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Lyfnua 45mg tablets
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA).
Active and completed clinical studies from ClinicalTrials.gov
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Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
6-10 hours
Mechanism
Gefapixant is a selective antagonist of P2X3 receptors, with some activity against the P2X2/3 receptor subtype.
Food interactions
1 warning
Human targets
2 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
78%
The absolute bioavailability of gefapixant has not been evaluated but is estimated to be ≥78%.
[L48596]…
[L48596]…
Half-life
6-10 hours
The terminal half-life of gefapixant is 6-10 hours.
[L48591]
[L48591]
Protein binding
55%
Gefapixant exhibits relatively low protein binding (55%) in vitro, and thus drug-drug interactions resulting from protein displacement are not expected.
[L48596]…
[L48596]…
Volume of distribution
133.8 L
Based on population pharmacokinetic analyses, the estimated steady-state apparent volume of distribution is 133.8…
Metabolism
14%
Gefapixant is relatively minimally metabolized. Following oral administration, only 14% of the administered dose was recovered as metabolites in the urine and feces.…
Elimination
76.4%
Gefapixant is primarily eliminated via renal excretion.
[L48591]
Following a single oral radiolabeled dose in a healthy male subject, approximately 76.4%…
[L48591]
Following a single oral radiolabeled dose in a healthy male subject, approximately 76.4%…
Clearance
10.8 L/h
Population pharmacokinetic analyses integrating data from Phase 1, 2, and 3 data showed a geometric mean apparent clearance (Cl/F) of 10.8…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
It has been estimated that 5-10% of adults globally suffer from chronic cough, which is defined as a cough lasting longer than eight weeks.[L48601] A subset of these patients remain symptomatic despite thorough investigation and treatment, termed refractory chronic cough (RCC) if they have a cough that does not respond to conventional treatment or unexplained chronic cough (UCC) when no diagnosable cause for the cough can be determined.[L48596] Existing treatments for chronic cough have been associated with considerable side effects, in particular opioids such as [codeine] or [dextromethorphan].[L48596]
Gefapixant is a novel antagonist of the P2X3 receptor that works to reduce the cough reflex in patients with chronic cough. It received approval in both Japan and Switzerland in 2022 for the treatment of adult patients with RCC and UCC, and received subsequent approval in the EU in September 2023 for the same indications.[L48596][L48591] It is the first therapy to be approved for the treatment of RCC or UCC in the EU.[L48601]
Gefapixant is a novel antagonist of the P2X3 receptor that works to reduce the cough reflex in patients with chronic cough. It received approval in both Japan and Switzerland in 2022 for the treatment of adult patients with RCC and UCC, and received subsequent approval in the EU in September 2023 for the same indications.[L48596][L48591] It is the first therapy to be approved for the treatment of RCC or UCC in the EU.[L48601]
Properties:
solid
Avg. mass: 353.40 Da
DrugBank indication
Gefapixant is indicated in adult patients for the treatment of refractory or unexplained chronic cough.
[L48591]
[L48591]
Also known as(33)
Gefapixant
ATP receptor
P2X3
Purinergic receptor
ATP receptor
P2X2
Purinergic receptor
ATP-binding cassette sub-family B member 1
Dosage forms(1)
Tablet, film coated (Oral) — 45 mg
Molecular properties(19)
Drug interactions(113)
Known interactions with other medications. Always consult a healthcare professional.
The risk or severity of adverse effects can be increased when Gefapixant is combined with Nicotine.
Mecamylamine
Unknown severity
The risk or severity of adverse effects can be increased when Gefapixant is combined with Mecamylamine.
Pentolinium
Unknown severity
The risk or severity of adverse effects can be increased when Gefapixant is combined with Pentolinium.
Trimethaphan
Unknown severity
The risk or severity of adverse effects can be increased when Gefapixant is combined with Trimethaphan.
Hexamethonium
Unknown severity
The risk or severity of adverse effects can be increased when Gefapixant is combined with Hexamethonium.
Cyclopentamine
Unknown severity
The risk or severity of adverse effects can be increased when Gefapixant is combined with Cyclopentamine.
Methotrexate
Unknown severity
The protein binding of Methotrexate can be increased when combined with Gefapixant.
Ketoprofen
Unknown severity
The risk or severity of adverse effects can be increased when Ketoprofen is combined with Gefapixant.
Dexketoprofen
Unknown severity
The risk or severity of adverse effects can be increased when Dexketoprofen is combined with Gefapixant.
Cyclosporine
Unknown severity
The risk or severity of renal failure can be increased when Gefapixant is combined with Cyclosporine.
Insulin human
Unknown severity
The risk or severity of hypoglycemia can be increased when Gefapixant is combined with Insulin human.
Insulin lispro
Unknown severity
The risk or severity of hypoglycemia can be increased when Gefapixant is combined with Insulin lispro.
Insulin glargine
Unknown severity
The risk or severity of hypoglycemia can be increased when Gefapixant is combined with Insulin glargine.
Insulin pork
Unknown severity
The risk or severity of hypoglycemia can be increased when Gefapixant is combined with Insulin pork.
Troglitazone
Moderate
The therapeutic efficacy of Troglitazone can be increased when used in combination with Gefapixant.
Glimepiride
Moderate
The therapeutic efficacy of Glimepiride can be increased when used in combination with Gefapixant.
Sulfisoxazole
Moderate
The therapeutic efficacy of Sulfisoxazole can be increased when used in combination with Gefapixant.
Disopyramide
Moderate
The therapeutic efficacy of Disopyramide can be increased when used in combination with Gefapixant.
The therapeutic efficacy of Acarbose can be increased when used in combination with Gefapixant.
The therapeutic efficacy of Metformin can be increased when used in combination with Gefapixant.
Sulfadiazine
Moderate
The therapeutic efficacy of Sulfadiazine can be increased when used in combination with Gefapixant.
Rosiglitazone
Moderate
The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Gefapixant.
Acetohexamide
Moderate
The therapeutic efficacy of Acetohexamide can be increased when used in combination with Gefapixant.
The therapeutic efficacy of Quinine can be increased when used in combination with Gefapixant.
The therapeutic efficacy of Miglitol can be increased when used in combination with Gefapixant.
Chlorpropamide
Moderate
The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Gefapixant.
Nateglinide
Moderate
The therapeutic efficacy of Nateglinide can be increased when used in combination with Gefapixant.
Pentamidine
Moderate
The therapeutic efficacy of Pentamidine can be increased when used in combination with Gefapixant.
Mifepristone
Moderate
The therapeutic efficacy of Mifepristone can be increased when used in combination with Gefapixant.
Tolazamide
Moderate
The therapeutic efficacy of Tolazamide can be increased when used in combination with Gefapixant.
Repaglinide
Moderate
The therapeutic efficacy of Repaglinide can be increased when used in combination with Gefapixant.
Phenformin
Moderate
The therapeutic efficacy of Phenformin can be increased when used in combination with Gefapixant.
Sulfamethoxazole
Moderate
The therapeutic efficacy of Sulfamethoxazole can be increased when used in combination with Gefapixant.
The therapeutic efficacy of Glyburide can be increased when used in combination with Gefapixant.
The therapeutic efficacy of Glipizide can be increased when used in combination with Gefapixant.
Gliclazide
Moderate
The therapeutic efficacy of Gliclazide can be increased when used in combination with Gefapixant.
Tolbutamide
Moderate
The therapeutic efficacy of Tolbutamide can be increased when used in combination with Gefapixant.
Pioglitazone
Moderate
The therapeutic efficacy of Pioglitazone can be increased when used in combination with Gefapixant.
Bromocriptine
Moderate
The therapeutic efficacy of Bromocriptine can be increased when used in combination with Gefapixant.
Gliquidone
Moderate
The therapeutic efficacy of Gliquidone can be increased when used in combination with Gefapixant.
Mitiglinide
Moderate
The therapeutic efficacy of Mitiglinide can be increased when used in combination with Gefapixant.
Sitagliptin
Moderate
The therapeutic efficacy of Sitagliptin can be increased when used in combination with Gefapixant.
The therapeutic efficacy of Sunitinib can be increased when used in combination with Gefapixant.
The therapeutic efficacy of Exenatide can be increased when used in combination with Gefapixant.
Mecasermin
Moderate
The therapeutic efficacy of Mecasermin can be increased when used in combination with Gefapixant.
Pramlintide
Moderate
The therapeutic efficacy of Pramlintide can be increased when used in combination with Gefapixant.
Glisoxepide
Moderate
The therapeutic efficacy of Glisoxepide can be increased when used in combination with Gefapixant.
Insulin aspart
Unknown severity
The risk or severity of hypoglycemia can be increased when Gefapixant is combined with Insulin aspart.
Insulin detemir
Unknown severity
The risk or severity of hypoglycemia can be increased when Gefapixant is combined with Insulin detemir.
Insulin glulisine
Unknown severity
The risk or severity of hypoglycemia can be increased when Gefapixant is combined with Insulin glulisine.
Showing 50 of 113 interactions
Food & lifestyle interactions
Advice
Take with or without food. The administration of gefapixant with food does not result in clinically significant differences in its pharmacokinetics.
Toxicity & overdose
In a clinical study in which 8 healthy subjects were administered gefapixant 1800 mg twice daily (40 times greater than the recommended dose) for up to 14 days, participants were found to have crystallized gefapixant in the urine with no additional evidence of renal or urinary system injury.
[L48591]
[L48591]
How it works
Mechanism of action
Gefapixant is a selective antagonist of P2X3 receptors, with some activity against the P2X2/3 receptor subtype.[L48591]
P2X3 receptors are ATP-gated ion channels found on sensory C fibers of the vagus nerve in the airways. Under inflammatory conditions, ATP is released from airway mucosal cells where it can subsequently bind to P2X3 receptors on C fibers. The activation of vagal C fibers is perceived as an urge to cough and initiates a cough reflex.[L48591] Gefapixant inhibits the binding of ATP to P2X3 receptors, thereby reducing excessive C fiber activation by extracellular ATP and dampening the subsequent cough reflex.[L48591]
P2X3 receptors are ATP-gated ion channels found on sensory C fibers of the vagus nerve in the airways. Under inflammatory conditions, ATP is released from airway mucosal cells where it can subsequently bind to P2X3 receptors on C fibers. The activation of vagal C fibers is perceived as an urge to cough and initiates a cough reflex.[L48591] Gefapixant inhibits the binding of ATP to P2X3 receptors, thereby reducing excessive C fiber activation by extracellular ATP and dampening the subsequent cough reflex.[L48591]
Pharmacodynamics
Gefapixant exerts its therapeutic effects via suppressing the cough reflex initiated by sensory C fibers of the vagus nerve.[L48591] In clinical studies, patients experienced a significant reduction in 24-hour cough frequency compared to placebo - this reduction was apparent by Week 4 and persisted throughout the remainder of the primary efficacy period.[L48591]
As renal excretion is the primary route of elimination for gefapixant, patients with severe renal impairment (eGFR < 30 mL/min/1.73m2) may require dose adjustment to maintain appropriate systemic exposures.[L48591]
As renal excretion is the primary route of elimination for gefapixant, patients with severe renal impairment (eGFR < 30 mL/min/1.73m2) may require dose adjustment to maintain appropriate systemic exposures.[L48591]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
The absolute bioavailability of gefapixant has not been evaluated but is estimated to be ≥78%.
[L48596]
At the recommended dose of 45 mg twice daily, steady-state is achieved within 2 days and the steady-state mean plasma AUC and Cmax are 4,144 ng∙hr/mL and 531 ng/mL, respectively.
[L48591]
The time to peak plasma concentration (Tmax) following oral administration ranges from one to four hours.
[L48591]
The co-administration of gefapixant with a high-fat, high-calorie meal had no effect on its AUC or Cmax.
[L48591]
[L48596]
At the recommended dose of 45 mg twice daily, steady-state is achieved within 2 days and the steady-state mean plasma AUC and Cmax are 4,144 ng∙hr/mL and 531 ng/mL, respectively.
[L48591]
The time to peak plasma concentration (Tmax) following oral administration ranges from one to four hours.
[L48591]
The co-administration of gefapixant with a high-fat, high-calorie meal had no effect on its AUC or Cmax.
[L48591]
Half-life
The terminal half-life of gefapixant is 6-10 hours.
[L48591]
[L48591]
Protein binding
Gefapixant exhibits relatively low protein binding (55%) in vitro, and thus drug-drug interactions resulting from protein displacement are not expected.
[L48596]
[L48596]
Volume of distribution
Based on population pharmacokinetic analyses, the estimated steady-state apparent volume of distribution is 133.8 L (Vc 101 L and Vp 32.8 L) following oral twice-daily administration of gefapixant 45 mg.
[L48596]
[L48596]
Metabolism
Gefapixant is relatively minimally metabolized. Following oral administration, only 14% of the administered dose was recovered as metabolites in the urine and feces. Unchanged parent drug is the major (87%) drug-related component in plasma, with circulating metabolites accounting for <10% each.
[L48591]
The primary biotransformation pathways observed in gefapixant ADME studies included hydroxylation, O-demethylation, dehydrogenation, oxidation, and direct glucuronidation.
Secondary biotransformation pathways included glucuronidation of O-demethylated metabolite as well as the formation of a metabolite that was O-demethylated and hydrogenated.
[L48596]
The three most abundant circulating metabolites were: M1 (a glucuronide of O-demethylated gefapixant), M5 (a directly glucuronidated parent) and M13 (a hydroxylated metabolite.), which accounted for 1.0%, 6.3%, and 5.8%, respectively, of the total drug-related components in plasma.
[L48596]
[L48591]
The primary biotransformation pathways observed in gefapixant ADME studies included hydroxylation, O-demethylation, dehydrogenation, oxidation, and direct glucuronidation.
Secondary biotransformation pathways included glucuronidation of O-demethylated metabolite as well as the formation of a metabolite that was O-demethylated and hydrogenated.
[L48596]
The three most abundant circulating metabolites were: M1 (a glucuronide of O-demethylated gefapixant), M5 (a directly glucuronidated parent) and M13 (a hydroxylated metabolite.), which accounted for 1.0%, 6.3%, and 5.8%, respectively, of the total drug-related components in plasma.
[L48596]
Route of elimination
Gefapixant is primarily eliminated via renal excretion.
[L48591]
Following a single oral radiolabeled dose in a healthy male subject, approximately 76.4% of the administered radioactivity was recovered in the urine and 22.6% was recovered in the feces.
[L48596][A261896]
Unchanged parent drug accounted for 64% of the recovered dose in the feces and accounted for 20% of the recovered dose in the urine.
[L48596][A261896]
[L48591]
Following a single oral radiolabeled dose in a healthy male subject, approximately 76.4% of the administered radioactivity was recovered in the urine and 22.6% was recovered in the feces.
[L48596][A261896]
Unchanged parent drug accounted for 64% of the recovered dose in the feces and accounted for 20% of the recovered dose in the urine.
[L48596][A261896]
Clearance
Population pharmacokinetic analyses integrating data from Phase 1, 2, and 3 data showed a geometric mean apparent clearance (Cl/F) of 10.8 L/h.
[L48596]
In clinical pharmacology studies, the observed clearance was 14.8 L/h and renal clearance was approximately 8.7 L/h.
[L48596]
[L48596]
In clinical pharmacology studies, the observed clearance was 14.8 L/h and renal clearance was approximately 8.7 L/h.
[L48596]
Drug targets(2)
Proteins and enzymes this drug interacts with in the body
P2X purinoceptor 3
P2RX3
antagonist
inhibitor
Specific functionATP binding
Cellular location
Cell membrane
General function & pharmacology
Extracellular ATP-activated non-selective cation channel .
PMID:10440098 PMID:27626375 PMID:29674445 PMID:31232692
Plays particularly important role in sensory neurons where its activation is critical for gustatory, nociceptive responses, visceral reflexes and sensory hypersensitization (By similarity)
PMID:10440098 PMID:27626375 PMID:29674445 PMID:31232692
Plays particularly important role in sensory neurons where its activation is critical for gustatory, nociceptive responses, visceral reflexes and sensory hypersensitization (By similarity)
P2X purinoceptor 2
P2RX2
antagonist
Specific functionATP binding
Cellular location
Cell membrane
General function & pharmacology
ATP-gated nonselective transmembrane cation channel permeable to potassium, sodium and calcium .
PMID:10570044 PMID:31636190
Activation by extracellular ATP induces a variety of cellular responses, such as excitatory postsynaptic responses in sensory neurons, neuromuscular junctions (NMJ) formation, hearing, perception of taste and peristalsis (By similarity). In the inner ear, regulates sound transduction and auditory neurotransmission, outer hair cell electromotility, inner ear gap junctions, and K(+) recycling .
PMID:23345450
Mediates synaptic transmission between neurons and from neurons to smooth muscle (By similarity)
PMID:10570044 PMID:31636190
Activation by extracellular ATP induces a variety of cellular responses, such as excitatory postsynaptic responses in sensory neurons, neuromuscular junctions (NMJ) formation, hearing, perception of taste and peristalsis (By similarity). In the inner ear, regulates sound transduction and auditory neurotransmission, outer hair cell electromotility, inner ear gap junctions, and K(+) recycling .
PMID:23345450
Mediates synaptic transmission between neurons and from neurons to smooth muscle (By similarity)
Transporters(4)
Proteins that transport this drug across cell membranes
ATP-dependent translocase ABCB1
ABCB1
substrate
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Translocates drugs and phospholipids across the membrane .
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
Multidrug and toxin extrusion protein 1
SLC47A1
substrate
Specific functionantiporter activity
Cellular location
Cell membrane
General function & pharmacology
Multidrug efflux pump that functions as a H(+)/organic cation antiporter .
PMID:16330770 PMID:17509534
Plays a physiological role in the excretion of cationic compounds including endogenous metabolites, drugs, toxins through the kidney and liver, into urine and bile respectively .
PMID:16330770 PMID:17495125 PMID:17509534 PMID:17582384 PMID:18305230 PMID:19158817 PMID:21128598 PMID:24961373
Mediates the efflux of endogenous compounds such as creatinine, vitamin B1/thiamine, agmatine and estrone-3-sulfate .
PMID:16330770 PMID:17495125 PMID:17509534 PMID:17582384 PMID:18305230 PMID:19158817 PMID:21128598 PMID:24961373
May also contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (Probable)
PMID:16330770 PMID:17509534
Plays a physiological role in the excretion of cationic compounds including endogenous metabolites, drugs, toxins through the kidney and liver, into urine and bile respectively .
PMID:16330770 PMID:17495125 PMID:17509534 PMID:17582384 PMID:18305230 PMID:19158817 PMID:21128598 PMID:24961373
Mediates the efflux of endogenous compounds such as creatinine, vitamin B1/thiamine, agmatine and estrone-3-sulfate .
PMID:16330770 PMID:17495125 PMID:17509534 PMID:17582384 PMID:18305230 PMID:19158817 PMID:21128598 PMID:24961373
May also contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (Probable)
Multidrug and toxin extrusion protein 2
SLC47A2
substrate
Specific functionantiporter activity
Cellular location
Cell membrane
General function & pharmacology
Multidrug efflux pump that functions as a H(+)/organic cation antiporter. Mediates the efflux of cationic compounds, such as the model cations, tetraethylammonium (TEA) and 1-methyl-4-phenylpyridinium (MPP+), the platinum-based drug oxaliplatin or weak bases that are positively charged at physiological pH, cimetidine, the platinum-based drugs cisplatin and oxaliplatin or the antidiabetic drug metformin. Mediates the efflux of endogenous compounds such as, creatinine, thiamine and estrone-3-sulfate.
Plays a physiological role in the excretion of drugs, toxins and endogenous metabolites through the kidney
Plays a physiological role in the excretion of drugs, toxins and endogenous metabolites through the kidney
Broad substrate specificity ATP-binding cassette transporter ABCG2
ABCG2
substrate
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells .
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
Scientific references(1)
Nussbaum J.C., Hussain A., Ma B., Min K.C., Chen Q., Tomek C., Iwamoto M., Stoch S.A.
Characterization of the absorption, metabolism, excretion, and mass balance of gefapixant in humans.
Pharmacology Research Perspect
2022 Feb10(1):e00924. doi: 10.1002/prp2.924
ATC classification(2 codes)
ATC R05DB29
ATC G01AE10
Affected organisms(1)
Humans
Salt forms(1)
Gefapixant citrate(DBSALT003486)
Experimental properties(1)
Protein Data Bank entries(1)
Commercial products(4)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Gefapixant
Additional database identifiers
ChemSpider
58828660
BindingDB
50533006
PDB
AF9
ZINC
ZINC000116342482
HUGO Gene Nomenclature Committee (HGNC)
HGNC:8534
GeneCards
P2RX3
Guide to Pharmacology
480
UniProt Accession
P2RX3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:15459
GeneCards
P2RX2
Guide to Pharmacology
479
UniProt Accession
P2RX2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:25588
GeneCards
SLC47A1
GenBank Gene Database
AK001709
GenBank Protein Database
7023138
Guide to Pharmacology
1216
UniProt Accession
S47A1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:26439
GeneCards
SLC47A2
Guide to Pharmacology
1217
UniProt Accession
S47A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:74
GenAtlas
ABCG2
GeneCards
ABCG2
GenBank Gene Database
AF103796
GenBank Protein Database
4185796
Guide to Pharmacology
792
UniProt Accession
ABCG2_HUMAN
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated about 1 month ago(4 Mar 2026)