Public dataset
Recorded enzyme and transporter findings by polarity
Inspect every admitted source sentence for an exact medicine, enzyme or transporter, and recorded role, with assertions, denials, and unresolved polarity counted separately.
- Public rows
- 8,404
- Generated
- Schema version
- 1.3.0
Coverage
What this run contains
- Medicine–counterparty–role groups
- 8,404
- Source sentence records
- 20,358
- Asserted sentences
- 4,700
- Denied sentences
- 7,494
- Polarity not recorded
- 8,164
- Medicines represented
- 755
- Counterparties represented
- 36
- Corpus records considered
- 9,855
- All corpus records were checked; a record without a documented counterparty cannot produce a row in this projection.
- inducer groups
- 617
- inhibitor groups
- 3,131
- not_recorded groups
- 3,074
- substrate groups
- 1,582
Method
How the rows were made
- A deterministic parser reads recorded FDA-label excerpts for named enzymes and transporters.
- A mention is admitted only when the stored excerpt contains the recorded counterparty, allowing letter-case differences only.
- Every admitted mention is grouped by exact medicine slug, recorded counterparty spelling, and exact role. A missing role remains NOT_RECORDED rather than being assigned to another group.
- Each sentence carries the exact source version and effective date when recorded; the API serializes null and the page says not recorded when either is absent.
- The API paginates groups. Within each returned group, sentences is the complete untruncated list used by the three polarity counts.
Limits
Read these before using a row
- A recorded role is a mechanistic statement copied from a descriptive label section. It is not a clinical interaction, and nothing in this dataset describes what happens when a person is exposed to two medicines at once.
- This dataset holds no relation between one medicine and another. Counts are per counterparty; the medicines naming a counterparty are listed with their sentences and are never paired, ranked against each other or compared.
- ICH M12 states that no potency classification system exists for transporters or for non-CYP enzymes, so no strong, moderate or weak vocabulary is applied to any counterparty here. The tallies count records, not strength.
- A counterparty with a high count is one that labels document often. Documentation frequency is not importance: US labelling asks for some enzymes to be characterised far more routinely than others, and that requirement is part of what these counts measure.
- 40.1% of admitted mentions carry no role. The sentence named more than one role and the parser left the question open rather than attaching a guess, so a role tally is a count of sentences that settled the question, not of medicines for which it is settled.
- Recorded spellings are counted separately and never merged. P-GP, PGP and P-GLYCOPROTEIN are three entries in this dataset because they are three strings in the corpus; whether they name one thing is a question for a person, and prefix relationships are reported as questions rather than resolved.
- 9088 of 9855 records name no enzyme or transporter at all. That is an absence of recorded text in the sources fetched for those records. It is neither reassurance nor alarm about the medicines concerned.
- 20358 of 20358 admitted mentions come from records the deterministic label parser produced, where no person chose the value or wrote its measurement context. The sentence is stored with each one so a reader can check it.
- The uniform reference for concentration allocates the same 20358 mentions over the same 36 counterparties by chance. Labels are not written that way, so the reference shows only that the observed spread is not a consequence of how many mentions there are.
- The public rows enumerate documentation about one medicine and one named counterparty. They never create medicine-to-medicine pairs and cannot answer whether two medicines interact.
- A NOT_RECORDED role or polarity remains unresolved. It is never folded into an assertion or a denial.
- Each returned group includes every admitted source sentence for checking, but the full source document remains authoritative.
Provenance
Source examples
Abacavir · CYP3A4 inhibitor
2 asserted · 2 denied · 0 polarity not recorded
FDA_LABEL:5676d391-f9a4-44be-9604-954b3d8d0e2b (opens source in a new tab)In vitro experiments reveal that abacavir does not inhibit human CYP3A4, CYP2D6, or CYP2C9 activity at clinically relevant concentrations.
Abacavir · BCRP substrate
0 asserted · 4 denied · 0 polarity not recorded
FDA_LABEL:5676d391-f9a4-44be-9604-954b3d8d0e2b (opens source in a new tab)Based on in vitro study results, abacavir at therapeutic drug exposures is not expected to affect the pharmacokinetics of drugs that are substrates of the following transporters: organic anion transporter polypeptide (OATP)1B1/3, breast cancer resistance protein (BCRP) or P-glycoprotein (P-gp), organic cation transporter (OCT)1, OCT2, or multidrug and toxic extrusion protein (MATE)1 and MATE2-K.
Abacavir · CYP2C9 not_recorded
0 asserted · 0 denied · 2 polarity not recorded
FDA_LABEL:5676d391-f9a4-44be-9604-954b3d8d0e2b (opens source in a new tab)Abacavir did not inhibit or induce other CYP enzymes (such as CYP2C9, or CYP2D6).
Artifact used for this view: data/agents/current/enzyme-and-transporter-documentation.json. The reader resolves the current run first and uses the checked-in compatibility run only when a current artifact is absent.
Schema
Fields in the public projection
| Field | Type | Meaning |
|---|---|---|
| medicineSlug | string | Stable RNAWiki medicine route key. |
| medicineName | string | Recorded medicine name; not normalized for display style. |
| counterparty | string | The exact recorded counterparty spelling. |
| role | string | SUBSTRATE, INHIBITOR, INDUCER, or NOT_RECORDED when the sentence did not settle one role. |
| assertedCount | number | Sentence records whose polarity is ASSERTED. |
| deniedCount | number | Sentence records whose polarity is NEGATED. |
| polarityNotRecordedCount | number | Sentence records for which the parser did not settle assertion or denial. |
| sentences | sentence[] | Every admitted sentence for this group, with polarity, section, source identity, source version/effective date or explicit absence, retrieval date, and exact excerpt. The list is not truncated. |
Reader
Search and filter the rows
Showing 3,061–3,070 of 8,404 matching rows. Filters and search terms remain attached when you move between pages or open the API view.
Projected row 3061
- Medicine slug
- fentanyl
- Medicine name
- Fentanyl
- Enzyme or transporter
- CYP3A4
- Role
- INDUCER
- Asserted sentences
- 2
- Denied sentences
- 0
- Polarity not recorded
- 0
- Complete sentence records
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:bf02ffd0-cc5d-446b-b648-378f6885052f (opens source in a new tab)
Fentanyl label
Version not recorded · Effective date not recorded
CYP3A4 Inducers Co-administration with agents that induce CYP3A4 activity may reduce the efficacy of fentanyl transdermal system.
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:bf02ffd0-cc5d-446b-b648-378f6885052f (opens source in a new tab)
Fentanyl label
Version not recorded · Effective date not recorded
CYP3A4 Inducers Co-administration with agents that induce CYP3A4 activity may reduce the efficacy of fentanyl transdermal system.
Projected row 3062
- Medicine slug
- fentanyl
- Medicine name
- Fentanyl
- Enzyme or transporter
- CYP3A4
- Role
- INHIBITOR
- Asserted sentences
- 6
- Denied sentences
- 0
- Polarity not recorded
- 0
- Complete sentence records
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:bf02ffd0-cc5d-446b-b648-378f6885052f (opens source in a new tab)
Fentanyl label
Version not recorded · Effective date not recorded
Drug Interaction Studies CYP3A4 Inhibitors Fentanyl is metabolized mainly via the human cytochrome P450 3A4 isoenzyme system (CYP3A4).
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:bf02ffd0-cc5d-446b-b648-378f6885052f (opens source in a new tab)
Fentanyl label
Version not recorded · Effective date not recorded
The interaction between ritonavir, a CYP3A4 inhibitor, and fentanyl was investigated in eleven healthy volunteers in a randomized crossover study.
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:bf02ffd0-cc5d-446b-b648-378f6885052f (opens source in a new tab)
Fentanyl label
Version not recorded · Effective date not recorded
Carefully monitor patients receiving fentanyl transdermal system and any CYP3A4 inhibitor for signs of respiratory depression for an extended period of time and adjust the dosage if warranted [see Boxed Warning and Warnings and Precautions ( 5.7 ), and Drug Interactions ( 7 )].
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:bf02ffd0-cc5d-446b-b648-378f6885052f (opens source in a new tab)
Fentanyl label
Version not recorded · Effective date not recorded
Drug Interaction Studies CYP3A4 Inhibitors Fentanyl is metabolized mainly via the human cytochrome P450 3A4 isoenzyme system (CYP3A4).
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:bf02ffd0-cc5d-446b-b648-378f6885052f (opens source in a new tab)
Fentanyl label
Version not recorded · Effective date not recorded
The interaction between ritonavir, a CYP3A4 inhibitor, and fentanyl was investigated in eleven healthy volunteers in a randomized crossover study.
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:bf02ffd0-cc5d-446b-b648-378f6885052f (opens source in a new tab)
Fentanyl label
Version not recorded · Effective date not recorded
Carefully monitor patients receiving fentanyl transdermal system and any CYP3A4 inhibitor for signs of respiratory depression for an extended period of time and adjust the dosage if warranted [see Boxed Warning and Warnings and Precautions ( 5.7 ), and Drug Interactions ( 7 )].
Projected row 3063
- Medicine slug
- fesoterodine
- Medicine name
- Fesoterodine
- Enzyme or transporter
- CYP1A2
- Role
- NOT_RECORDED
- Asserted sentences
- 0
- Denied sentences
- 0
- Polarity not recorded
- 2
- Complete sentence records
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Drug-Drug Interactions Drugs Metabolized by Cytochrome P450 At therapeutic concentrations, the active metabolite of fesoterodine does not inhibit CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A4, or induce CYP1A2, 2B6, 2C9, 2C19, or 3A4 in vitro [see Drug Interactions ( 7.5 )] .
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Drug-Drug Interactions Drugs Metabolized by Cytochrome P450 At therapeutic concentrations, the active metabolite of fesoterodine does not inhibit CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A4, or induce CYP1A2, 2B6, 2C9, 2C19, or 3A4 in vitro [see Drug Interactions ( 7.5 )] .
Projected row 3064
- Medicine slug
- fesoterodine
- Medicine name
- Fesoterodine
- Enzyme or transporter
- CYP2D6
- Role
- INHIBITOR
- Asserted sentences
- 4
- Denied sentences
- 0
- Polarity not recorded
- 0
- Complete sentence records
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
CYP3A4 Inhibitors Following blockade of CYP3A4 by coadministration of the strong CYP3A4 inhibitor ketoconazole 200 mg twice a day for 5 days, C max and AUC of the active metabolite of fesoterodine increased 2- and 2.3-fold, respectively, after oral administration of fesoterodine fumarate 8 mg to CYP2D6 extensive metabolizers.
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
In poor metabolizers for CYP2D6, representing a maximum CYP2D6 inhibition, C max and AUC of the active metabolite are increased 1.7- and 2-fold, respectively [see Drug Interactions ( 7.4 ) ] .
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
CYP3A4 Inhibitors Following blockade of CYP3A4 by coadministration of the strong CYP3A4 inhibitor ketoconazole 200 mg twice a day for 5 days, C max and AUC of the active metabolite of fesoterodine increased 2- and 2.3-fold, respectively, after oral administration of fesoterodine fumarate 8 mg to CYP2D6 extensive metabolizers.
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
In poor metabolizers for CYP2D6, representing a maximum CYP2D6 inhibition, C max and AUC of the active metabolite are increased 1.7- and 2-fold, respectively [see Drug Interactions ( 7.4 ) ] .
Projected row 3065
- Medicine slug
- fesoterodine
- Medicine name
- Fesoterodine
- Enzyme or transporter
- CYP2D6
- Role
- NOT_RECORDED
- Asserted sentences
- 0
- Denied sentences
- 0
- Polarity not recorded
- 23
- Complete sentence records
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
A summary of pharmacokinetic parameters for the active metabolite after a single dose of fesoterodine fumarate 4 mg and 8 mg in extensive and poor metabolizers of CYP2D6 is provided in Table 8.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
The active metabolite is further metabolized in the liver to its carboxy, carboxy-N-desisopropyl, and N-desisopropyl metabolites via two major pathways involving CYP2D6 and CYP3A4.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Variability in CYP2D6 Metabolism A subset of individuals (approximately 7% of Caucasians and approximately 2% of African Americans) are poor metabolizers for CYP2D6.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
C max and AUC of the active metabolite are increased 1.7- and 2-fold, respectively, in CYP2D6 poor metabolizers, as compared to extensive metabolizers.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Pediatric Patients In pediatric patients, from 6 years to 17 years of age with NDO weighing 35 kg with CYP2D6 extensive metabolizer status receiving fesoterodine tablets, the mean values of apparent oral clearance, volume of distribution and absorption rate constant of 5-HMT are estimated to be approximately 72 L/h, 68 L and 0.09 h-1, respectively.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Like adults, the 5-HMT exposures in CYP2D6 poor metabolizers was estimated to be approximately 2-fold higher compared with extensive metabolizers.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
In CYP2D6 poor metabolizers, C max and AUC of the active metabolite of fesoterodine increased 2.1- and 2.5-fold, respectively, during coadministration of ketoconazole 200 mg twice a day for 5 days.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
C max and AUC were 4.5- and 5.7-fold higher, respectively, in subjects who were CYP2D6 poor metabolizers and taking ketoconazole compared to subjects who were CYP2D6 extensive metabolizers and not taking ketoconazole.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
In a separate study coadministering fesoterodine with ketoconazole 200 mg once a day for 5 days, the C max and AUC values of the active metabolite of fesoterodine were increased 2.2-fold in CYP2D6 extensive metabolizers and 1.5- and 1.9-fold, respectively, in CYP2D6 poor metabolizers.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
C max and AUC were 3.4-and 4.2-fold higher, respectively, in subjects who were CYP2D6 poor metabolizers and taking ketoconazole compared to subjects who were CYP2D6 extensive metabolizers and not taking ketoconazole.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
CYP2D6 Inhibitors The interaction with CYP2D6 inhibitors was not studied.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Fesoterodine 28 mg was chosen because this dose, when administered to CYP2D6 extensive metabolizers, results in an exposure to the active metabolite that is similar to the exposure in a CYP2D6 poor metabolizer receiving fesoterodine 8 mg together with CYP3A4 blockade.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
A summary of pharmacokinetic parameters for the active metabolite after a single dose of fesoterodine fumarate 4 mg and 8 mg in extensive and poor metabolizers of CYP2D6 is provided in Table 8.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
The active metabolite is further metabolized in the liver to its carboxy, carboxy-N-desisopropyl, and N-desisopropyl metabolites via two major pathways involving CYP2D6 and CYP3A4.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Variability in CYP2D6 Metabolism A subset of individuals (approximately 7% of Caucasians and approximately 2% of African Americans) are poor metabolizers for CYP2D6.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
C max and AUC of the active metabolite are increased 1.7- and 2-fold, respectively, in CYP2D6 poor metabolizers, as compared to extensive metabolizers.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Pediatric Patients In pediatric patients, from 6 years to 17 years of age with NDO weighing 35 kg with CYP2D6 extensive metabolizer status receiving fesoterodine tablets, the mean values of apparent oral clearance, volume of distribution and absorption rate constant of 5-HMT are estimated to be approximately 72 L/h, 68 L and 0.09 h-1, respectively.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Like adults, the 5-HMT exposures in CYP2D6 poor metabolizers was estimated to be approximately 2-fold higher compared with extensive metabolizers.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
In CYP2D6 poor metabolizers, C max and AUC of the active metabolite of fesoterodine increased 2.1- and 2.5-fold, respectively, during coadministration of ketoconazole 200 mg twice a day for 5 days.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
C max and AUC were 4.5- and 5.7-fold higher, respectively, in subjects who were CYP2D6 poor metabolizers and taking ketoconazole compared to subjects who were CYP2D6 extensive metabolizers and not taking ketoconazole.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
In a separate study coadministering fesoterodine with ketoconazole 200 mg once a day for 5 days, the C max and AUC values of the active metabolite of fesoterodine were increased 2.2-fold in CYP2D6 extensive metabolizers and 1.5- and 1.9-fold, respectively, in CYP2D6 poor metabolizers.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
C max and AUC were 3.4-and 4.2-fold higher, respectively, in subjects who were CYP2D6 poor metabolizers and taking ketoconazole compared to subjects who were CYP2D6 extensive metabolizers and not taking ketoconazole.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
CYP2D6 Inhibitors The interaction with CYP2D6 inhibitors was not studied.
Projected row 3066
- Medicine slug
- fesoterodine
- Medicine name
- Fesoterodine
- Enzyme or transporter
- CYP3A4
- Role
- INDUCER
- Asserted sentences
- 4
- Denied sentences
- 2
- Polarity not recorded
- 0
- Complete sentence records
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
CYP3A4 Inducers Following induction of CYP3A4 by coadministration of rifampicin 600 mg once a day, C max and AUC of the active metabolite of fesoterodine decreased by approximately 70% and 75%, respectively, after oral administration of fesoterodine fumarate 8 mg.
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Induction of CYP3A4 may lead to reduced plasma levels.
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
CYP3A4 Inducers Following induction of CYP3A4 by coadministration of rifampicin 600 mg once a day, C max and AUC of the active metabolite of fesoterodine decreased by approximately 70% and 75%, respectively, after oral administration of fesoterodine fumarate 8 mg.
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Induction of CYP3A4 may lead to reduced plasma levels.
- NEGATEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
No dosing adjustments are recommended in the presence of CYP3A4 inducers [see Drug Interactions ( 7.3 )] .
- NEGATEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
No dosing adjustments are recommended in the presence of CYP3A4 inducers [see Drug Interactions ( 7.3 )] .
Projected row 3067
- Medicine slug
- fesoterodine
- Medicine name
- Fesoterodine
- Enzyme or transporter
- CYP3A4
- Role
- INHIBITOR
- Asserted sentences
- 4
- Denied sentences
- 2
- Polarity not recorded
- 0
- Complete sentence records
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
CYP3A4 Inhibitors Following blockade of CYP3A4 by coadministration of the strong CYP3A4 inhibitor ketoconazole 200 mg twice a day for 5 days, C max and AUC of the active metabolite of fesoterodine increased 2- and 2.3-fold, respectively, after oral administration of fesoterodine fumarate 8 mg to CYP2D6 extensive metabolizers.
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
In a drug-drug interaction study evaluating the coadministration of the moderate CYP3A4 inhibitor fluconazole 200 mg twice a day for 2 days, a single 8 mg dose of fesoterodine was administered 1 hour following the first dose of fluconazole on day 1 of the study.
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
CYP3A4 Inhibitors Following blockade of CYP3A4 by coadministration of the strong CYP3A4 inhibitor ketoconazole 200 mg twice a day for 5 days, C max and AUC of the active metabolite of fesoterodine increased 2- and 2.3-fold, respectively, after oral administration of fesoterodine fumarate 8 mg to CYP2D6 extensive metabolizers.
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
In a drug-drug interaction study evaluating the coadministration of the moderate CYP3A4 inhibitor fluconazole 200 mg twice a day for 2 days, a single 8 mg dose of fesoterodine was administered 1 hour following the first dose of fluconazole on day 1 of the study.
- NEGATEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
There is no clinically relevant effect of moderate CYP3A4 inhibitors on the pharmacokinetics of fesoterodine.
- NEGATEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
There is no clinically relevant effect of moderate CYP3A4 inhibitors on the pharmacokinetics of fesoterodine.
Projected row 3068
- Medicine slug
- fesoterodine
- Medicine name
- Fesoterodine
- Enzyme or transporter
- CYP3A4
- Role
- NOT_RECORDED
- Asserted sentences
- 0
- Denied sentences
- 0
- Polarity not recorded
- 5
- Complete sentence records
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
The active metabolite is further metabolized in the liver to its carboxy, carboxy-N-desisopropyl, and N-desisopropyl metabolites via two major pathways involving CYP2D6 and CYP3A4.
- NOT_RECORDEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
The effect of weak CYP3A4 inhibitors (e.g., cimetidine) was not examined; it is not expected to be in excess of the effect of moderate inhibitors [see Drug Interactions (7.2) and Dosage and Administration ( 2.2 , 2.3 )] .
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
Fesoterodine 28 mg was chosen because this dose, when administered to CYP2D6 extensive metabolizers, results in an exposure to the active metabolite that is similar to the exposure in a CYP2D6 poor metabolizer receiving fesoterodine 8 mg together with CYP3A4 blockade.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
The active metabolite is further metabolized in the liver to its carboxy, carboxy-N-desisopropyl, and N-desisopropyl metabolites via two major pathways involving CYP2D6 and CYP3A4.
- NOT_RECORDEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:8c68e918-b47b-466d-80bc-4f521aa74607 (opens source in a new tab)
Fesoterodine label
Version not recorded · Effective date not recorded
The effect of weak CYP3A4 inhibitors (e.g., cimetidine) was not examined; it is not expected to be in excess of the effect of moderate inhibitors [see Drug Interactions (7.2) and Dosage and Administration ( 2.2 , 2.3 )] .
Projected row 3069
- Medicine slug
- fexinidazole
- Medicine name
- Fexinidazole
- Enzyme or transporter
- BCRP
- Role
- INHIBITOR
- Asserted sentences
- 0
- Denied sentences
- 2
- Polarity not recorded
- 0
- Complete sentence records
- NEGATEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:74a611bc-9977-46bb-b626-0370b3031628 (opens source in a new tab)
Fexinidazole label
Version not recorded · Effective date not recorded
Fexinidazole, M1, or M2 do not inhibit P-gp or BCRP.
- NEGATEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:74a611bc-9977-46bb-b626-0370b3031628 (opens source in a new tab)
Fexinidazole label
Version not recorded · Effective date not recorded
Fexinidazole, M1, or M2 do not inhibit P-gp or BCRP.
Projected row 3070
- Medicine slug
- fexinidazole
- Medicine name
- Fexinidazole
- Enzyme or transporter
- CYP1A2
- Role
- INDUCER
- Asserted sentences
- 4
- Denied sentences
- 0
- Polarity not recorded
- 0
- Complete sentence records
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:74a611bc-9977-46bb-b626-0370b3031628 (opens source in a new tab)
Fexinidazole label
Version not recorded · Effective date not recorded
Fexinidazole has the potential to induce CYP1A2 and CYP2B6.
- ASSERTEDpharmacokineticsRetrieved 2026-08-30FDA_LABEL:74a611bc-9977-46bb-b626-0370b3031628 (opens source in a new tab)
Fexinidazole label
Version not recorded · Effective date not recorded
Metabolite M1 has the potential to induce CYP1A2, CYP2B6, CYP3A5, UGT1A4, UGT2B4 and UGT2B7.
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:74a611bc-9977-46bb-b626-0370b3031628 (opens source in a new tab)
Fexinidazole label
Version not recorded · Effective date not recorded
Fexinidazole has the potential to induce CYP1A2 and CYP2B6.
- ASSERTEDclinical_pharmacologyRetrieved 2026-08-30FDA_LABEL:74a611bc-9977-46bb-b626-0370b3031628 (opens source in a new tab)
Fexinidazole label
Version not recorded · Effective date not recorded
Metabolite M1 has the potential to induce CYP1A2, CYP2B6, CYP3A5, UGT1A4, UGT2B4 and UGT2B7.
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