Tolterodine is a muscarinic receptor antagonist used to treat overactive bladder with urinary incontinence, urgency, and frequency. Tolterodine acts on M2 and M3 subtypes of muscarinic receptors.
- Mechanism
- Curator reviewed
Both tolterodine and its active metabolite, 5-hydroxymethyltolterodine, act as competitive antagonists at muscarinic receptors. This antagonism results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.
- Primary indication
- For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).Curator reviewed · 1 structured indication
- Formula / weight
- C22H31NO · 325.4876 g/mol (avg)
- First approval
- Canada, 2011 · United States, 1998
- Brand names
Resolves to
Clinical / RWD
Structure
InChIKey
OOGJQPCLVADCPB-HXUWFJFHSA-NSMILESCC(C)N(CC[C@H](C1=CC=CC=C1)C1=C(O)C=CC(C)=C1)C(C)CWhat you can answer from here — as of September 23, 2026
5Protein targetsEach mapped to UniProt, with action and pharmacological actionListed above
Which drugs share a target with Tolterodine, and which of those have an active Phase 3 trial?
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