Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
ZYDELIG vs FASTIN
Clinician-reviewed, head-to-head comparison of mechanism, dosing, pharmacokinetics, and safety profiles.
Last clinically reviewed: July 2026 · OpiCalc Medical Review Team
Idelalisib is a selective inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ), blocking the PI3K/AKT signaling pathway, leading to reduced proliferation, survival, and migration of malignant B cells.
Sympathomimetic amine that promotes release of norepinephrine and dopamine from presynaptic nerve terminals in the hypothalamus, suppressing appetite.
Relapsed chronic lymphocytic leukemia (CLL) in combination with rituximab,Relapsed follicular B-cell non-Hodgkin lymphoma (FL) in patients who have received at least two prior systemic therapies,Relapsed small lymphocytic lymphoma (SLL) in patients who have received at least two prior systemic therapies
Short-term adjunct in exogenous obesity,Off-label: Attention deficit hyperactivity disorder (ADHD)
150 mg orally twice daily, taken with food.
30 mg orally once daily in the morning, administered as a single dose.
Terminal elimination half-life is 6.5 hours (range 4-10 hours) after oral administration, supporting twice-daily dosing.
Terminal elimination half-life is approximately 16-20 hours for the immediate-release formulation. With sustained-release forms, effective half-life may extend to 24-34 hours due to prolonged absorption. Clinical context: time to reach steady state is about 3-5 days.
Primarily metabolized by aldehyde oxidase (AO) and CYP3A4, with minor contributions from UGT1A4.
Hepatic metabolism via CYP3A4 and CYP2D6; active metabolite phendimetrazine (for some formulations).
Primarily hepatic metabolism, with 44% of dose excreted in feces (as metabolites) and 22% in urine (unchanged drug and metabolites).
Primarily renal (approximately 70-80% unchanged) and biliary/fecal (20-30% as metabolites). Urinary excretion is p H-dependent; acidic urine increases elimination.
84% bound to plasma proteins, primarily to albumin and alpha-1-acid glycoprotein.
Approximately 40-50% bound to plasma proteins (albumin).
Mean volume of distribution is 113 L (approximately 1.4 L/kg), indicating extensive tissue distribution.
Approximately 3-5 L/kg. High Vd indicates extensive tissue distribution, including brain.
Absolute oral bioavailability is 40% (range 30-50%) due to first-pass metabolism.
Oral immediate-release: ~90% (high first-pass metabolism; absolute bioavailability is lower, but systemic exposure is adequate). Oral sustained-release: similar extent but with prolonged absorption.
No dose adjustment required for mild to moderate renal impairment (Cr Cl ≥30 m L/min). For severe renal impairment (Cr Cl <30 m L/min), not recommended due to lack of data.
Contraindicated in severe renal impairment (e GFR <30 m L/min/1.73 m²). For moderate impairment (e GFR 30-59 m L/min/1.73 m²), reduce dose to 15 mg once daily.
Child-Pugh Class A: No dose adjustment. Child-Pugh Class B: Reduce dose to 100 mg twice daily. Child-Pugh Class C: Not recommended.
Contraindicated in Child-Pugh class C cirrhosis. In Child-Pugh class A or B, initiate at 15 mg once daily and titrate cautiously to maximum 30 mg once daily.
Safety and efficacy not established for patients <18 years.
Not recommended for pediatric patients under 16 years of age due to lack of safety and efficacy data.
No specific dose adjustment recommended, but monitor for age-related renal and hepatic function changes.
Initiating at 15 mg once daily is recommended due to increased sensitivity and potential for central nervous system adverse effects; maximum dose 30 mg once daily.
WARNING: FATAL AND SERIOUS TOXICITIES: Hepatic, severe diarrhea/colitis, pneumonitis, and intestinal perforation. Fatal and/or serious hepatotoxicity occurred in 18% of patients. Fatal and/or serious diarrhea or colitis occurred in 14%. Fatal and/or serious pneumonitis occurred in 4%. Fatal and/or serious intestinal perforation occurred in <1%.
None.
Hepatotoxicity: Monitor liver function tests,Severe diarrhea/colitis: Manage with supportive care and corticosteroids,Pneumonitis: Interrupt therapy and evaluate,Intestinal perforation: Discontinue if suspected,Infections: Monitor for opportunistic infections, including CMV,Neutropenia: Monitor blood counts,Embryofetal toxicity: Can cause fetal harm,Vaccinations: Avoid live vaccines during treatment
Cardiovascular events (hypertension, tachycardia, stroke), psychiatric adverse effects (psychosis, dependence), primary pulmonary hypertension, valvular heart disease, tolerance, withdrawal symptoms, glaucoma, hyperthyroidism, seizure disorder, diabetes (dose adjustment required), elderly patients (higher sensitivity).
History of severe hypersensitivity (e.g., anaphylaxis, Stevens-Johnson syndrome) to idelalisib or any excipient
Cardiovascular disease (e.g., coronary artery disease, arrhythmias, hypertension), hyperthyroidism, glaucoma, agitated states, history of drug abuse, MAOIs (concurrent or within 14 days), hypersensitivity to sympathomimetics.
Avoid grapefruit and grapefruit juice (CYP3A4 inhibition increases idelalisib exposure). Take with food to reduce nausea and diarrhea.
Avoid excessive caffeine intake (e.g., coffee, tea, cola, energy drinks) as it may potentiate CNS and cardiovascular effects. Grapefruit juice may alter drug metabolism; avoid concurrent consumption. Maintain a balanced, reduced-calorie diet as part of the weight loss plan. Alcohol should be avoided due to potential additive CNS effects.
Pregnancy Category D. First trimester: Risk of fetal malformations including neural tube defects and craniofacial anomalies based on animal studies showing embryo-fetal toxicity and teratogenicity. Second and third trimesters: Risk of fetal hematologic toxicity (leukopenia, neutropenia) and potential growth restriction. Counsel women of childbearing age to use effective contraception during treatment and for 1 month after last dose.
FDA Pregnancy Category X. First trimester: Increased risk of oral clefts and cardiac malformations with amphetamine use. Second and third trimesters: Risk of premature delivery, low birth weight, and neonatal withdrawal syndrome. Avoid use in pregnancy.
No human data on presence in breast milk; risk of serious adverse reactions in breastfed infants (immunosuppression, neutropenia). M/P ratio not determined. Advise not to breastfeed during treatment and for 1 week after last dose.
Excreted in human milk; M/P ratio not established. Potential for adverse effects in nursing infants (irritability, poor feeding). Contraindicated during breastfeeding.
No dose adjustment studies in pregnant women. Due to increased volume of distribution and altered clearance in pregnancy, therapeutic drug monitoring is not established. Use minimum effective dose. If used during pregnancy, monitor for maternal neutropenia, infections, and adjust dose per standard ANC thresholds (hold if ANC < 500/mm³; resume at reduced dose when ANC > 1000/mm³).
Contraindicated in pregnancy; no dose adjustments recommended.
Monitor for hepatotoxicity (ALT/AST elevations), severe cutaneous reactions (Stevens-Johnson syndrome), and pneumonitis. Requires hepatic function monitoring every 2 weeks for first 2 months, then monthly. Contraindicated with CYP3A4 inducers or strong inhibitors due to metabolism via CYP3A4. Dose reduction needed for moderate hepatic impairment (Child-Pugh B).
Fastin (phentermine) is a sympathomimetic amine indicated for short-term (up to 12 weeks) monotherapy for obesity. It should be used in conjunction with a reduced-calorie diet and exercise. Avoid co-administration with MAOIs or within 14 days of MAOI use due to hypertensive crisis risk. Use with caution in patients with hypertension, diabetes, or history of drug abuse. Monitor blood pressure and heart rate regularly. Tachyphylaxis may develop; discontinue if tolerance occurs. Do not use in patients with advanced arteriosclerosis, hyperthyroidism, glaucoma, or agitated states.
Take with food to reduce gastrointestinal side effects.,Avoid grapefruit and grapefruit juice during treatment.,Report any signs of liver problems (jaundice, dark urine, abdominal pain) or skin reactions (rash, blisters) immediately.,Use effective contraception during and for at least 1 month after treatment.,Do not stop or change dose without consulting your healthcare provider.
Take Fastin exactly as prescribed, usually once daily in the morning to avoid insomnia.,Do not crush or chew the extended-release capsule; swallow whole.,Avoid taking late in the day to prevent difficulty sleeping.,Report any chest pain, palpitations, shortness of breath, or dizziness immediately.,Do not increase dose or take more frequently than prescribed; risk of dependence and side effects.,Fastin is for short-term use only (up to 12 weeks) and should be combined with a reduced-calorie diet and exercise.,Do not use if you have taken an MAO inhibitor in the last 14 days.,Avoid alcohol and other CNS stimulants (e.g., caffeine in large amounts) as they may increase side effects.,Do not stop abruptly; follow your doctor's instructions for tapering off.,Keep out of reach of children; misuse can cause severe cardiac toxicity.
No interactions on record
No interactions on record
Explore head-to-head clinical comparisons of other medications in the same therapeutic classes.
Common clinical questions about ZYDELIG vs FASTIN, answered by our medical review team.
ZYDELIG is a PI3K Inhibitor Antineoplastic that works by Idelalisib is a selective inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ), blocking the PI3K/AKT signaling pathway, leading to reduced proliferation, survival, and migration of malignant B cells.. FASTIN is a Sympathomimetic Anorectic that works by Sympathomimetic amine that promotes release of norepinephrine and dopamine from presynaptic nerve terminals in the hypothalamus, suppressing appetite.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between ZYDELIG and FASTIN depend on the specific clinical indication. These are agents from distinct pharmacological classes and are not directly interchangeable by dose. A physician or clinical pharmacist should guide any therapeutic switching decisions.
The standard adult dose of ZYDELIG is: 150 mg orally twice daily, taken with food.. The standard adult dose of FASTIN is: 30 mg orally once daily in the morning, administered as a single dose.. 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 ZYDELIG and FASTIN 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. ZYDELIG is classified as Category C. Pregnancy Category D. First trimester: Risk of fetal malformations including neural tube defects and craniofacial anomalies based on animal studies showing embryo-fetal toxicity an. FASTIN is classified as Category C. FDA Pregnancy Category X. First trimester: Increased risk of oral clefts and cardiac malformations with amphetamine use. Second and third trimesters: Risk of premature delivery, lo. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.