Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE vs AURLUMYN
Clinician-reviewed, head-to-head comparison of mechanism, dosing, pharmacokinetics, and safety profiles.
Last clinically reviewed: July 2026 · OpiCalc Medical Review Team
Trifluridine is a thymidine-based nucleoside analog that incorporates into DNA, interfering with DNA synthesis and function. Tipiracil hydrochloride inhibits thymidine phosphorylase, preventing trifluridine degradation and increasing its systemic exposure.
Microtubule inhibitor that binds to tubulin and disrupts microtubule dynamics, leading to mitotic arrest and apoptosis.
Metastatic colorectal cancer (m CRC) previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy.,Metastatic gastric or gastroesophageal junction adenocarcinoma previously treated with at least two prior lines of therapy including a fluoropyrimidine, a platinum, either a taxane or irinotecan, and if appropriate, HER2/neu-targeted therapy.
Treatment of relapsed or refractory multiple myeloma,Treatment of relapsed or refractory mantle cell lymphoma
35 mg/m² orally twice daily on days 1-5 and 8-12 of each 28-day cycle. Maximum dose: 80 mg per dose.
Intravenous, 6 mg/kg every 4 weeks for 6 cycles; each cycle: Days 1 and 15 of a 28-day cycle.
The terminal elimination half-life of trifluridine is approximately 1.4 to 2.1 hours. For tipiracil, the half-life is about 2.1 to 3.3 hours. The short half-lives necessitate twice-daily dosing to maintain therapeutic concentrations.
Terminal elimination half-life is 12-15 hours in patients with normal renal function; prolonged to 30-40 hours in severe renal impairment (Cr Cl <30 m L/min).
Trifluridine is primarily metabolized by thymidine phosphorylase to 5-(trifluoromethyl)uracil (inactive). Tipiracil is metabolized mainly via hepatic carboxylesterases and aldehyde oxidase, not significantly via CYP enzymes.
Primarily metabolized by CYP3A4 and to a lesser extent by CYP1A2 and CYP2C8.
Trifluridine is primarily eliminated via metabolism and renal excretion. Approximately 29% of the trifluride dose is recovered in urine as trifluridine and its metabolites, with less than 3% as unchanged drug. Fecal excretion accounts for about 38% of the dose, mainly as metabolites. Tipiracil is predominantly excreted renally (about 55% as unchanged drug and metabolites) and fecally (about 19%).
Primarily renal excretion of unchanged drug (60-70%) with biliary/fecal elimination accounting for 20-30%.
Trifluridine: <1% bound to plasma proteins. Tipiracil: about 8% bound to plasma proteins.
Approximately 85-90% bound to serum albumin.
Trifluridine: Vd/F is approximately 0.4 ± 0.1 L/kg, indicating distribution into total body water. Tipiracil: Vd/F is about 0.3 ± 0.1 L/kg.
0.5 L/kg, indicating distribution primarily into extracellular fluid with limited tissue penetration.
Following oral administration of the combination tablet, trifluridine has an absolute bioavailability of approximately 57% (fasted). Tipiracil bioavailability is about 70% (fasted). Food may alter absorption.
Oral bioavailability is 50-60% due to first-pass metabolism and incomplete absorption.
For GFR 30-59 m L/min: reduce dose to 20 mg/m² twice daily. For GFR 15-29 m L/min: reduce dose to 15 mg/m² twice daily. Contraindicated if GFR <15 m L/min.
GFR ≥30 m L/min: no adjustment. GFR <30 m L/min: not recommended (no data).
Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 25 mg/m² twice daily. Child-Pugh C: not recommended.
Child-Pugh A: no adjustment. Child-Pugh B or C: not recommended (no data).
Not established. Safety and efficacy in pediatric patients have not been studied.
Not established; safety and efficacy not determined in pediatric patients.
No specific dose adjustment recommended; monitor renal function and adjust based on renal impairment. Elderly patients may have increased risk of myelosuppression and infections.
No specific dose adjustment; monitor renal function and hematologic toxicity more frequently.
WARNING: NEUTROPENIA/THROMBOCYTOPENIA; AND GASTROINTESTINAL TOXICITY Neutropenia/Thrombocytopenia: Severe and life-threatening neutropenia and thrombocytopenia can occur. Obtain complete blood counts prior to each cycle and as clinically indicated. Withhold, reduce, or discontinue dosing for severe neutropenia or thrombocytopenia. Gastrointestinal Toxicity: Severe gastrointestinal toxicity including diarrhea, nausea, vomiting, and abdominal pain can occur. Withhold, reduce, or discontinue dosing for severe gastrointestinal toxicity.
None.
Bone Marrow Suppression: May cause severe neutropenia, thrombocytopenia, and anemia. Monitor blood counts.,Gastrointestinal Toxicity: Severe diarrhea, nausea, vomiting, abdominal pain, and stomatitis. Manage with supportive care.,Renal Toxicity: Proteinuria, nephrotic syndrome. Monitor renal function.,Hepatic Toxicity: Elevations of liver enzymes and bilirubin. Monitor liver function.,Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential of effective contraception and avoid breastfeeding.
Hematologic toxicity (neutropenia, thrombocytopenia, anemia), infection risk, peripheral neuropathy, cardiotoxicity (heart failure), embryo-fetal toxicity.
None reported in prescribing information. Use caution in patients with severe renal impairment (Cr Cl <30 m L/min) or severe hepatic impairment.
Hypersensitivity to AURLUMYN or any of its components.
Take within 1 hour after a meal (breakfast and dinner) to reduce variability and improve tolerability. Avoid grapefruit or grapefruit juice? No established interaction; however, general caution due to potential CYP3A4 involvement? (minimal). High-fat meals may reduce peak concentration but do not significantly alter overall exposure; timing with meals is recommended not for efficacy but to mitigate gastrointestinal side effects.
Avoid alcohol. No specific food interactions, but maintain a balanced diet. Take with food or milk if gastrointestinal upset occurs.
Trifluridine/tipiracil is embryotoxic and teratogenic in animal studies. In humans, avoid use during pregnancy; effective contraception required during treatment and for at least 6 months after last dose. First trimester: highest risk of major malformations; second and third trimesters: risk of fetal growth restriction and adverse neonatal outcomes.
First trimester: Increased risk of major congenital malformations (neural tube defects, cardiovascular anomalies) based on animal studies and limited human data. Second and third trimesters: Risk of fetal growth restriction, oligohydramnios, and preterm birth. Avoid in pregnancy unless benefit outweighs risk.
No human data on excretion in breast milk. Based on drug properties, likely present; advise against breastfeeding during treatment and for at least 1 day after last dose. M/P ratio unknown.
No data on excretion in human milk; M/P ratio unknown. Due to potential for serious adverse reactions in breastfed infants, breastfeeding is not recommended during treatment and for at least 2 weeks after last dose.
No established dose adjustments for pregnancy; avoid use. Pharmacokinetic changes in pregnancy (increased volume of distribution, clearance) may alter exposure, but no data to guide adjustment.
No specific dosing adjustments established for pregnancy. Pregnancy-induced pharmacokinetic changes (increased volume of distribution, enhanced renal clearance) may reduce drug exposure; consider therapeutic drug monitoring if available.
Tipiracil hydrochloride/trifluridine (Lonsurf) is a combination oral cytotoxic agent used for refractory metastatic colorectal cancer and gastric cancer. Trifluridine incorporates into DNA, inhibiting thymidylate synthase; tipiracil inhibits trifluridine degradation by thymidine phosphorylase. Administer within 1 hour after morning and evening meals to reduce variation in exposure. Avoid severe neutropenia by monitoring CBCs before and after each cycle; hold for ANC <500/mm³ or febrile neutropenia. Use antiemetics as needed; nausea/vomiting occur in ~50% of patients. Dose reduction recommended for severe myelosuppression, including thrombocytopenia and anemia. No strong CYP interactions; avoid concurrent use of UGT1A1 or thymidine phosphorylase inhibitors? (limited data). Consider growth factor support for prolonged neutropenia.
AURLUMYN is a proprietary name for auranofin, an oral gold compound used for rheumatoid arthritis. Monitor for oral ulcerations, dermatitis, and proteinuria. Renal function and CBC should be checked monthly. Avoid concurrent use with penicillamine, antimalarials, immunosuppressants, or cytotoxic drugs. Onset of action may be delayed 3-6 months.
Take each dose with a glass of water within 1 hour after breakfast and dinner; do not crush or chew tablets.,Swallow tablets whole; do not take if vomiting occurs after a dose—skip that dose and resume next scheduled dose.,Store at room temperature away from moisture and heat; keep bottle tightly closed.,Common side effects include nausea, vomiting, diarrhea, loss of appetite, fatigue, and low blood cell counts.,Contact healthcare provider immediately if fever, signs of infection (sore throat, cough), unusual bleeding/bruising, or severe tiredness occur.,Use effective contraception during treatment and for at least 6 months after the last dose for females and 3 months for males.,Avoid handling crushed or broken tablets; if contact occurs, wash skin thoroughly.,Do not breastfeed during treatment and for at least 1 day after last dose.
Take exactly as prescribed; do not adjust dose without consulting your doctor.,Report any mouth sores, skin rash, unexplained bruising, or change in urine color immediately.,Regular blood and urine tests are required to monitor for side effects.,May take 3-6 months to feel full benefit; do not stop suddenly.,Avoid alcohol as it may increase risk of liver toxicity.,Use effective contraception during treatment and for 6 months after stopping.,Do not take any other medications (including OTC) without approval from your doctor.
"Tipiracil, a component of the combination chemotherapeutic agent Lonsurf (with trifluridine), inhibits thymidine phosphorylase and can also inhibit organic cation transporter 2 (OCT2). Pramipexole, a dopamine agonist used for Parkinson's disease and restless legs syndrome, is primarily eliminated renally via active tubular secretion mediated by OCT2. When coadministered, Tipiracil reduces the renal clearance of Pramipexole by inhibiting OCT2, leading to increased plasma concentrations of Pramipexole. This elevates the risk of dose-dependent adverse effects such as orthostatic hypotension, hallucinations, somnolence, and impulse control disorders."
"Tipiracil inhibits thymidine phosphorylase, which is involved in the metabolism of prazosin, leading to reduced clearance and increased systemic exposure of prazosin. This can result in enhanced alpha-adrenergic blockade, causing profound hypotension, dizziness, and syncope, especially during initial dosing or dose escalation."
"The serum concentration of Histamine can be increased when it is combined with Tipiracil."
No interactions on record
Explore head-to-head clinical comparisons of other medications in the same therapeutic classes.
Common clinical questions about TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE vs AURLUMYN, answered by our medical review team.
TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE is a Antineoplastic Agent that works by Trifluridine is a thymidine-based nucleoside analog that incorporates into DNA, interfering with DNA synthesis and function. Tipiracil hydrochloride inhibits thymidine phosphorylase, preventing trifluridine degradation and increasing its systemic exposure.. AURLUMYN is a Antineoplastic Agent that works by Microtubule inhibitor that binds to tubulin and disrupts microtubule dynamics, leading to mitotic arrest and apoptosis.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE and AURLUMYN depend on the specific clinical indication. These are both Antineoplastic Agent agents and are not directly interchangeable by dose. A physician or clinical pharmacist should guide any therapeutic switching decisions.
The standard adult dose of TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE is: 35 mg/m² orally twice daily on days 1-5 and 8-12 of each 28-day cycle. Maximum dose: 80 mg per dose.. The standard adult dose of AURLUMYN is: Intravenous, 6 mg/kg every 4 weeks for 6 cycles; each cycle: Days 1 and 15 of a 28-day cycle.. Dosing should always be individualized based on indication, renal and hepatic function, age, and other patient factors.
No direct drug-drug interaction has been formally documented between TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE and AURLUMYN in current clinical databases. However, individual patient risk factors including other medications, organ function, and comorbidities should always be evaluated by a qualified healthcare provider.
The maternal-fetal safety profiles differ. TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE is classified as Category C. Trifluridine/tipiracil is embryotoxic and teratogenic in animal studies. In humans, avoid use during pregnancy; effective contraception required during treatment and for at least 6. AURLUMYN is classified as Category C. First trimester: Increased risk of major congenital malformations (neural tube defects, cardiovascular anomalies) based on animal studies and limited human data. Second and third t. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.