JIDEYTRO zidesamtinib 25 mg Tablet, Film Coated, 30-count
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🧪 Inactive Ingredients / Excipients
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UNII 1K09F3G675
Ferric oxide red is an inorganic iron compound used as a colorant in medicines. It gives tablets, capsules, or other dosage forms a red or reddish tint for identification and appearance.
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UNII EX438O2MRT
Ferric oxide yellow is a naturally occurring iron compound used as a colorant in medications. It gives tablets, capsules, and other forms a yellow or golden hue for identification and appearance.
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UNII UKE75GEA7F
Hydroxypropyl cellulose is a plant-based polymer used as a binder and thickener. It helps hold tablet ingredients together, controls how fast the medicine dissolves, and improves the texture of liquid formulations.
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UNII 0WZ8WG20P6
Hypromellose 2910 is a plant-based cellulose derivative that acts as a thickener, binder, and film-coating agent. It helps control how quickly the medicine dissolves and protects the tablet or capsule from moisture and light.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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UNII 3OWL53L36A
A natural sugar alcohol derived from seaweed or synthesized in the lab. It's used as a filler to add bulk, a sweetener in sugar-free formulas, and a disintegrant to help tablets break apart in the stomach.
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UNII 88X4A2YW6T
A plant-based powder made from cellulose mixed with silica. It works as a binder to hold tablet ingredients together and as a glidant to help the powder flow smoothly during manufacturing.
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UNII H8AV0SQX4D
A modified starch derived from potato or corn starch. It absorbs water quickly and helps tablets or capsules break apart and dissolve in the stomach, acting as a disintegrant to ensure the medicine releases its active ingredients properly.
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UNII 15FIX9V2JP
Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
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UNII XHX3C3X673
Triacetin is a clear, oily liquid made from glycerin and acetic acid. It works as a plasticizer and solvent in medicines, helping soften coatings and improve how liquids mix together in formulations.
10 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Jideytro 25 mgthis 85001-0101-01 | Nuvalent, | 30 tablets | — | — | FDA listed | — |
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⏳ Availability & generic status
We did not find an FDA-approved generic match for this exact strength, form and route.
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 85001-0101-01 You're viewing this | 1 BOTTLE in 1 CARTON (85001-101-01) / 30 TABLET, FILM COATED in 1 BOTTLE | 2026-07-22 | Active |
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| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | — Not published for this NDC Applies only to products approved under an NDA/ANDA; many listings are out of scope. |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE JIDEYTRO is indicated for the treatment of adult patients with locally advanced or metastatic ROS1 -positive non-small cell lung cancer (NSCLC) who received a prior ROS1 kinase inhibitor [see Dosage and Administration ( 2.1 ), Clinical Studies ( 14.1 )] . JIDEYTRO is a kinase inhibitor indicated for the treatment of adult patients with locally advanced or metastatic ROS1 -positive non-small cell lung cancer (NSCLC) who received a prior ROS1 kinase inhibitor.( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Recommended Dosage : 100 mg orally once daily with or without food until disease progression or unacceptable toxicity. ( 2.2 )
2.1Recommended Testing and Evaluation Before Initiating JIDEYTRO Before initiating JIDEYTRO, evaluate creatine phosphokinase (CPK) level, electrocardiogram (ECG), electrolytes, lipase and amylase [see Warnings and Precautions ( 5.2 , 5.5 , 5.6 )] .
2.2Recommended Dosage The recommended dosage of JIDEYTRO is 100 mg taken orally once daily, with or without food, until disease progression or unacceptable toxicity [see Clinical Pharmacology ( 12.3 )] . Swallow JIDEYTRO tablets whole. Do not split, chew, crush, or dissolve the tablet prior to swallowing.
Missed Dose If a dose of JIDEYTRO is missed within 12 hours of the regularly scheduled dose, administer the missed dose as soon as possible. If a dose is missed by 12 hours or more, take the next dose at its scheduled time. Vomiting If vomiting occurs at any time after taking JIDEYTRO, take the next dose at its scheduled time.
2.3Dosage Modifications of JIDEYTRO for Adverse Reactions The recommended dosage reductions of JIDEYTRO for the management of adverse reactions are provided in Table 1 . Table 1: Recommended Dose Reductions for JIDEYTRO Adverse Reactions Dose Reduction Recommended Dose and Schedule First 75 mg once daily Second 50 mg once daily Permanently discontinue JIDEYTRO in patients unable to tolerate 50 mg once daily. After dose reduction of JIDEYTRO for adverse reactions, do not re-escalate the dose.
The recommended dosage modifications of JIDEYTRO for the management of adverse reactions are provided in Table 2 . Table 2: Recommended Dosage Modifications for JIDEYTRO Adverse Reactions *Graded per National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE), version 5.0. Adverse Reaction Severity* Dosage Modification Central Nervous System Adverse Reactions [see Warnings and Precautions (5.1)] Intolerable Grade 2 Withhold JIDEYTRO until Grade ≤ 1 or baseline.
Resume JIDEYTRO at same or reduced dose, as clinically appropriate. Grade 3 Withhold JIDEYTRO until Grade ≤ 1 or baseline. Resume JIDEYTRO at reduced dose.
Grade 4 Permanently discontinue JIDEYTRO. QTc Interval Prolongation [see Warnings and Precautions ( 5.2 )] Grade 2 (QTc interval 481-500 msec) Withhold JIDEYTRO until recovery to Grade ≤ 1 or baseline. Correct electrolytes and/or change concomitant medications.
Resume JIDEYTRO at same dose. Grade 3 (QTc interval ≥501 msec or QTc interval increase of >60 msec from baseline) Withhold JIDEYTRO until recovery to Grade ≤ 1 or baseline. Correct electrolytes and/or change concomitant medications.
Resume JIDEYTRO at a reduced dose. Grade 4 (Torsade de pointes; polymorphic ventricular tachycardia; signs/symptoms of serious arrhythmia) Permanently discontinue JIDEYTRO. Interstitial Lung Disease (ILD)/Pneumonitis [see Warnings and Precautions (5.3)] Grade 1 Withhold JIDEYTRO if ILD/pneumonitis occurs or is suspected until recovery to Grade 0.
If resolved within 6 weeks, resume JIDEYTRO at the same dose. If unresolved after 6 weeks, permanently discontinue JIDEYTRO. Recurrence: Permanently discontinue JIDEYTRO.
Grade 2 Withhold JIDEYTRO if ILD/pneumonitis occurs or is suspected until recovery to Grade 0 or baseline. If resolved within 6 weeks, resume JIDEYTRO at a reduced dose. If unresolved after 6 weeks, permanently discontinue JIDEYTRO.
Recurrence: Permanently discontinue JIDEYTRO. Grade 3 or 4 Permanently discontinue JIDEYTRO. Creatine Phosphokinase (CPK) Elevation [see Warnings and Precautions (5.5)] CPK elevation > 5 times ULN Withhold JIDEYTRO until recovery to baseline or ≤ 2.5 times ULN, then resume JIDEYTRO at same dose.
CPK elevation > 10 times ULN or Recurrence of CPK elevation of >5 times ULN Withhold until recovery to baseline or ≤2.5 times ULN, then resume JIDEYTRO at a reduced dose. Increased lipase or amylase [see Warnings and Precautions (5.6)] Grade 3 Withhold JIDEYTRO until…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Tablets: 25 mg: pink, oblong, film-coated, debossed with "25" on one side and "ZDS" on the other side. Tablets: 100 mg: yellow, oblong, film-coated, debossed with "100" on one side and "ZDS" on the other side. Tablets: 25 mg and 100 mg.
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None.
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Central Nervous System (CNS) Adverse Reactions (AR): Can cause CNS AR including dizziness, ataxia, cognitive and psychiatric disorders. Based on severity, withhold JIDEYTRO and resume at same or reduced dose, or permanently discontinue. ( 5.1 ) QTc Interval Prolongation: Can cause QTc prolongation.
Evaluate ECGs and electrolytes prior to administration of JIDEYTRO and monitor periodically during treatment. Based on severity, withhold JIDEYTRO and resume at the same or reduced dose, or permanently discontinue. ( 5.2 ) Interstitial Lung Disease (ILD)/pneumonitis: Can cause ILD/pneumonitis.
Monitor patients for new or worsening pulmonary symptoms indicative of ILD/pneumonitis. Immediately withhold in patients with suspected ILD/pneumonitis. Based on severity, withhold JIDEYTRO and resume at the same or reduced dose, or permanently discontinue.
( 5.3 ) Skeletal Fractures : Can cause skeletal fractures. Promptly evaluate patients with signs or symptoms of fractures. ( 5.4 ) Myalgia with Creatine Phosphokinase (CPK) Elevation: Can cause CPK elevation.
Advise patients to report unexplained muscle pain or tenderness. Monitor serum CPK levels during treatment. Based on severity, withhold JIDEYTRO and resume at same or reduced dose upon recovery to baseline.
( 5.5 ) Pancreatic Toxicity: Evaluate amylase and lipase prior to administration of JIDEYTRO and monitor periodically during treatment. Withhold, dose reduce or permanently discontinue JIDEYTRO based on severity. ( 5.6 ) Embryo-Fetal Toxicity : Can cause fetal harm.
Advise patients of the potential risk to a fetus and to use effective contraception. ( 5.7 )
5.1Central Nervous System Adverse Reactions JIDEYTRO can cause central nervous system adverse reactions. In the pooled safety population [see Adverse Reactions ( 6.1) ] , a broad spectrum of central nervous system (CNS) adverse reactions, including dizziness, ataxia, cognitive and psychiatric disorders, occurred in 25% of patients who received JIDEYTRO; of these, 2.5% were Grade 3 or 4. One patient (0.2%) with brain metastases experienced a Grade 3 seizure.
Dizziness, including vertigo, presyncope and positional dizziness occurred in 12% of patients who received JIDEYTRO; of these 0.2% were Grade 3. The median time to onset of dizziness was 22 days (range: 1 day to 9 months). Dosage interruption of JIDEYTRO for dizziness was required in 0.4% of patients, and 0.7% of patients required dose reduction.
Ataxia, including gait disturbance and balance disorder, occurred in 2% of patients who received JIDEYTRO and were all Grade 1 or 2. The median time to onset of ataxia was 64 days (range: 6 days to 2.5 years). Cognitive impairment occurred in 9% of patients who received JIDEYTRO, of these 1.6% were Grade 3 or 4.
Cognitive impairment included memory impairment (3.1%), cognitive disorder (1.6%), hallucination (1.1%), delirium (1.1%), aphasia (0.9%), amnesia (0.7%), confusional state (0.7%), anterograde amnesia (0.2%), disturbance in attention (0.4%), slow speech (0.2%). The median time to onset of cognitive impairment was 43 days (range: 4 days to 1.9 years). Dose interruption of JIDEYTRO for cognitive impairment was required in 1.3% of patients.
Psychiatric disorders occurred in 6% of patients who received JIDEYTRO, of these 0.7% were Grade 3 or 4. Psychiatric disorders included anxiety (3.1%), depression (1.3%), agitation (0.7%), affect lability (0.4%), irritability (0.4%), abnormal behavior (0.2%), depressed mood (0.2%), personality change (0.2%), psychotic disorder (0.2%), and suicidal ideation (0.2%). The median time to onset of psychiatric disorders was 57 days (range: 1 day to 10 months).
Dosage interruption of JIDEYTRO for psychiatric disorders was required in 0.9% of patients. Advise patients and caregivers of the risk of CNS adverse reactions with JIDEYTRO. Advise patients to avoid engaging in hazardous tasks requiring mental alertness and motor coordination such as operating machinery or driving a…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Central Nervous System Adverse Reactions [see Warnings and Precautions ( 5.1 )] QTc Interval Prolongation [see Warnings and Precautions ( 5.2 )] Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions ( 5.3 )] Skeletal Fractures [see Warnings and Precautions ( 5.4 )] Myalgia with Creatine Phosphokinase Elevation [see Warnings and Precautions ( 5.5 )] Pancreatic Toxicity [see Warnings and Precautions ( 5.6 )] Most common adverse reactions (≥15%) were: edema, peripheral neuropathy, constipation, fatigue, and dyspnea.
( 6.1 ) Most common Grade 3 or 4 laboratory abnormalities (≥2%) were: increased CPK, increased triglycerides, decreased lymphocytes and decreased hemoglobin. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Nuvalent, Inc. at toll-free phone 1-844-NUVL-111 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The pooled safety population described in WARNINGS AND PRECAUTIONS reflects exposure to JIDEYTRO in 446 patients with ROS1-positive NSCLC (n=432) and other solid tumors (n=14) who received JIDEYTRO at a dose of 100 mg orally once daily until disease progression or unacceptable toxicity in ARROS-1 [see Clinical Studies ( 14.1 )] .
Among 446 patients who received JIDEYTRO, 44% were exposed for 6 months or longer and 14% were exposed for greater than one year. In this pooled safety population, the most common (≥15%) adverse reactions included: edema (38%), peripheral neuropathy (25%), constipation (17%), fatigue (16%), dyspnea (15%). The most common Grade 3 or 4 laboratory abnormalities (≥2%), were increased lipase (8%), increased creatine phosphokinase (CPK) (4%), increased triglycerides (3.5%), decreased lymphocytes (2.7%), and decreased hemoglobin (2.3%).
Previously Treated ROS1-positive NSCLC The safety of JIDEYTRO was evaluated in ARROS-1 [see Clinical Studies ( 14.1 )] . Patients received JIDEYTRO 100 mg orally once daily until disease progression or unacceptable toxicity. Among the 432 patients who received JIDEYTRO, 44% were exposed to JIDEYTRO for 6 months or longer, and 15% were exposed for greater than 1 year.
The median age of patients who received JIDEYTRO was 58 years (range: 26 to 87); 62% female; 41% White, 41% Asian, 3.7% Black or African American, 0.2% American Indian or Alaska Native, 14% other races, multiple races or race unknown, and 4.6% of patients were of Hispanic or Latino ethnicity. Serious adverse reactions occurred in 22% of patients who received JIDEYTRO. Serious adverse reactions in ≥2% of patients included pneumonia (6%) and dyspnea (2.5%).
Fatal adverse reactions occurred in 2.3% of patients who received JIDEYTRO, including pneumonia (0.5%), cerebrovascular accident (0.2%), COVID-19 (0.2%), dyspnea (0.2%), infectious pleural effusion (0.2%), influenza (0.2%), myocardial infarction (0.2%), myocarditis (0.2%), and respiratory failure (0.2%). Permanent discontinuation of JIDEYTRO due to an adverse reaction occurred in 2.3% of patients. Adverse reactions resulting in permanent discontinuation of JIDEYTRO occurring in ≥2 patients were pneumonia (0.7%) and pneumonitis (0.5%).
Dosage interruptions of JIDEYTRO due to an adverse reaction occurred in 30% of patients. Adverse reactions which required dosage interruption in ≥1% of patients included pneumonia (4.6%), increased creatine phosphokinase level (3.0%), peripheral neuropathy (1.9%), peripheral edema (1.6%), COVID-19 (1.4%), and dyspnea and elevated alanine aminotransferase level (each in 1.2%). Dose reductions of JIDEYTRO due to an adverse reaction occurred in 10% of patients.
Adverse reactions which required dosage r…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Strong and Moderate CYP3A Inhibitors: Avoid concomitant use. ( 7.1 ) Strong and Moderate CYP3A Inducers: Avoid concomitant use. ( 7.1 )
7.1Effects of Other Drugs on JIDEYTRO Strong and Moderate CYP3A Inhibitors Avoid concomitant use of JIDEYTRO with a strong or moderate CYP3A inhibitor. Zidesamtinib is a CYP3A substrate. Concomitant use with a strong or moderate CYP3A inhibitor increases zidesamtinib exposure [see Clinical Pharmacology ( 12.3 )] , which may increase the risk of JIDEYTRO adverse reactions.
Strong and Moderate CYP3A Inducers Avoid concomitant use of JIDEYTRO with strong or moderate CYP3A inducers. Concomitant use of JIDEYTRO with a strong or moderate CYP3A inducer may decrease zidesamtinib exposure [see Clinical Pharmacology ( 12.3 )], which may decrease the effectiveness of JIDEYTRO.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPUTLATIONS Lactation : Advise not to breastfeed. ( 8.2 ) Infertility: May impair fertility. ( 8.3 )
8.1Pregnancy Risk Summary Based on literature reports in humans with congenital mutations leading to changes in TRK signaling, findings from animal studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , JIDEYTRO can cause fetal harm when administered to a pregnant woman. There are no available data on JIDEYTRO use in pregnant women to inform a drug-associated risk. Oral administration of zidesamtinib to pregnant rats during the period of organogenesis resulted in embryo-fetal mortality, alterations to growth, and structural abnormalities at maternal exposures approximately equivalent to the human exposure at the recommended dose based on AUC ( see Data ).
Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Human Data Published reports of individuals with congenital mutations in TRK pathway proteins suggest that decreases in TRK mediated signaling are correlated with obesity, developmental delays, cognitive impairment, insensitivity to pain, and anhidrosis.
Animal Data In an embryo-fetal development study, pregnant rats received oral doses of 3, 8, or 30 mg/kg/day of zidesamtinib during the period of organogenesis (gestation day 6 to 17). Zidesamtinib caused decreased fetal body weight, visceral malformations (absent kidneys and ureter), and an increase in the incidence of skeletal variations, including misshapen sternebra and cervical arch and incomplete ossification of the sternebra and thoracic centrum at 3 mg/kg/day (approximately 1.4 times the human exposure at the recommended dose based on AUC).
Zidesamtinib resulted in complete litter resorption (post-implantation loss) at doses ≥8 mg/kg/day (approximately ≥3.5 times the human exposure at the recommended dose based on AUC).
8.2Lactation Risk Summary There are no data on the presence of JIDEYTRO in human milk or their effects on either a breastfed child or on milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with JIDEYTRO and for 1 week after the last dose.
8.3Females and Males of Reproductive Potential JIDEYTRO can cause fetal harm when administered to a pregnant woman [ see Use in Specific Populations ( 8.1 ) ]. Pregnancy Testing Verify the pregnancy status of females of reproductive potential prior to initiating JIDEYTRO [ see Use in Specific Populations ( 8.1 ) ]. Contraception Females Advise females of reproductive potential to use effective contraception during treatment with JIDEYTRO and for 6 months after the last dose.
Males Advise male patients with female partners of reproductive potential to use effective contraception during treatment with JIDEYTRO and for 3 months after the last dose [see Nonclinical Toxicology ( 13.1 ) ] . Infertility Based on findings from animal studies, JIDEYTRO may impair fertility in males and females. The effects on male fertility were reversible.
The reversibility of the effect on fertility in females is unknown [see Nonclinical Toxicology ( 13.1 ) ].
8.4Pediatric Use The safety and effectiveness of JIDEYTRO in pediatric patients has not been established. Juvenile Animal Data Daily oral administration of zidesamtinib to juvenile rats from postnatal day 7 to 28 (approximately equal to a human pediatric age of a neonate to child) resulted in ocular toxicity, including hemorrhage, corneal ulcers, rupture, and vision loss at 8 mg/kg/day (approximately 2.4 times the human exposure based on AUC at the recommended dose).
8.5Geriatric Use Of the 446 patients who received JIDEYTRO, 21.5% were 65 to 74 years old, and 8% were 75 years of age or older. There were no clinically meaningful differences in safety and efficacy betw…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Based on literature reports in humans with congenital mutations leading to changes in TRK signaling, findings from animal studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , JIDEYTRO can cause fetal harm when administered to a pregnant woman. There are no available data on JIDEYTRO use in pregnant women to inform a drug-associated risk. Oral administration of zidesamtinib to pregnant rats during the period of organogenesis resulted in embryo-fetal mortality, alterations to growth, and structural abnormalities at maternal exposures approximately equivalent to the human exposure at the recommended dose based on AUC ( see Data ).
Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Human Data Published reports of individuals with congenital mutations in TRK pathway proteins suggest that decreases in TRK mediated signaling are correlated with obesity, developmental delays, cognitive impairment, insensitivity to pain, and anhidrosis.
Animal Data In an embryo-fetal development study, pregnant rats received oral doses of 3, 8, or 30 mg/kg/day of zidesamtinib during the period of organogenesis (gestation day 6 to 17). Zidesamtinib caused decreased fetal body weight, visceral malformations (absent kidneys and ureter), and an increase in the incidence of skeletal variations, including misshapen sternebra and cervical arch and incomplete ossification of the sternebra and thoracic centrum at 3 mg/kg/day (approximately 1.4 times the human exposure at the recommended dose based on AUC).
Zidesamtinib resulted in complete litter resorption (post-implantation loss) at doses ≥8 mg/kg/day (approximately ≥3.5 times the human exposure at the recommended dose based on AUC).
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of JIDEYTRO in pediatric patients has not been established. Juvenile Animal Data Daily oral administration of zidesamtinib to juvenile rats from postnatal day 7 to 28 (approximately equal to a human pediatric age of a neonate to child) resulted in ocular toxicity, including hemorrhage, corneal ulcers, rupture, and vision loss at 8 mg/kg/day (approximately 2.4 times the human exposure based on AUC at the recommended dose).
🧓 Geriatric Use ▾
8.5Geriatric Use Of the 446 patients who received JIDEYTRO, 21.5% were 65 to 74 years old, and 8% were 75 years of age or older. There were no clinically meaningful differences in safety and efficacy between patients younger than 65 years of age and patients 65 years of age or older.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Zidesamtinib is an inhibitor of tyrosine kinase ROS1, including ROS1 resistance mutations. In a biochemical assay, zidesamtinib inhibited ROS1 (IC 50 = 0.7 nM) and also showed inhibitory effects on ALK (IC 50 = 3 nM) and tropomyosin receptor kinases (TRKs), TRKB (IC 50 = 54 nM), TRKC (IC 50 = 193 nM) and TRKA (IC 50 = 258 nM). In vitro, zidesamtinib inhibited the viability of cultured cells expressing ROS1 fusion genes and resistance mutations (G2032R, S1986F, F2004C/V, L2026M, D2033N, and G2101A).
In mice subcutaneously implanted with tumors harboring ROS1 fusions, including the G2032R mutation, administration of zidesamtinib resulted in tumor growth inhibition. Zidesamtinib had antitumor activity in an intracranial NSCLC xenograft model harboring a ROS1 fusion.
12.2Pharmacodynamics Exposure-Response Relationships An increased incidence of dysgeusia was observed with higher metabolite M9 exposure. Cardiac Electrophysiology The largest mean increase in QTc interval was 13 ms (upper confidence interval = 19 ms) after administration of JIDEYTRO 100 mg once daily (the maximum recommended dosage) in patients with advanced ROS1-positive NSCLC and other advanced ROS1-positive solid tumors [see Warnings and Precautions ( 5.2 )].
12.3Pharmacokinetics Zidesamtinib pharmacokinetics were observed at steady-state in patients with advanced ROS1-positive NSCLC and other solid tumors at the approved recommended dosage and are presented as mean (coefficient of variation [CV]%) unless otherwise specified. Zidesamtinib maximum plasma concentration (C max ) is 934 ng/mL (44%) and total systemic exposure (AUC) is 8,310 ng.h/mL (37%). Zidesamtinib C max and AUC increase in a dose proportional manner over the dose range of 25 mg to 100 mg orally once daily (0.25 to 1 times the maximum recommended dosage).
Zidesamtinib accumulation is approximately 1.5-fold and steady-state is reached in approximately 4 days. Absorption Zidesamtinib median (min, max) time to maximum plasma concentration (T max ) is 1 hour (0.3, 6 hours). Zidesamtinib absolute bioavailability is 83%.
Effect of Food No clinically significant differences in zidesamtinib exposure were observed in healthy participants following administration of a high fat meal (approximately 1,000 calories with 60% fat). Distribution Zidesamtinib apparent (oral) volume of distribution (V ss ) is 326 L (18%). Zidesamtinib plasma protein binding is 79% and is not concentration-dependent in vitro.
Zidesamtinib blood-to-plasma ratio was 0.9 in vitro. Elimination Zidesamtinib elimination half-life is 18 (51%) hours with an apparent (oral) clearance of 12 (37%) L/h. Metabolism Zidesamtinib is primarily metabolized by CYP3A with minor contributions from CYP1A2 and CYP2C8.
An active metabolite, a des-ethyl metabolite (M9), with activity one-third that of the parent, was identified in plasma and its AUC represents 48% of the parent AUC. Excretion Following oral administration of a single 100 mg radiolabeled dose to healthy participants, approximately 47% of the dose was recovered in the urine (< 1% unchanged) and 33% in the feces (< 2% as unchanged). Specific Populations No clinically meaningful differences in the pharmacokinetics of zidesamtinib were observed based on age (26 to 87 years), sex, race (White 44%, Asian 38%, or Black 4%), body weight (36 to 162 kg), eGFR 30 to 90 mL/min [estimated by Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI)], or mild (total bilirubin >1 to 1.5 times ULN or AST > ULN) to moderate (total bilirubin >1.5 to 3 times ULN with any AST) hepatic impairment.
The effect of severe (total bilirubin >3 x ULN with any AST) hepatic impairment, severe renal impairment (eGFR < 30 mL/min), or dialysis on zidesamtinib pharmacokinetics is unknown. Drug Interaction Studies Clinical Studies Strong CYP3A Inhibitors : Zidesamtinib AUC increased 2.6-fold and C max increased 1.8-fold following concomitant use of itraconazole (strong CYP3…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Zidesamtinib is an inhibitor of tyrosine kinase ROS1, including ROS1 resistance mutations. In a biochemical assay, zidesamtinib inhibited ROS1 (IC 50 = 0.7 nM) and also showed inhibitory effects on ALK (IC 50 = 3 nM) and tropomyosin receptor kinases (TRKs), TRKB (IC 50 = 54 nM), TRKC (IC 50 = 193 nM) and TRKA (IC 50 = 258 nM). In vitro, zidesamtinib inhibited the viability of cultured cells expressing ROS1 fusion genes and resistance mutations (G2032R, S1986F, F2004C/V, L2026M, D2033N, and G2101A).
In mice subcutaneously implanted with tumors harboring ROS1 fusions, including the G2032R mutation, administration of zidesamtinib resulted in tumor growth inhibition. Zidesamtinib had antitumor activity in an intracranial NSCLC xenograft model harboring a ROS1 fusion.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied JIDEYTRO (zidesamtinib) is supplied as follows: Tablet Strength Package Configuration Description NDC 25 mg Bottle of 30 tablets packaged in a carton Pink oblong film-coated tablet, with "25" debossed on one side and "ZDS" on the other side 85001-101-01 100 mg Bottle of 30 tablets packaged in a carton Yellow oblong film-coated tablet, with "100" debossed on one side and "ZDS" on the other side 85001-102-01 Storage and Handling Store JIDEYTRO at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [See USP Controlled Room Temperature] .
📋 Description ▾
11 DESCRIPTION Zidesamtinib is a kinase inhibitor. The molecular formula for zidesamtinib is C 22 H 22 FN 7 O and the molecular weight is 419.46 Daltons. The chemical name is ( R )-3-Ethyl-16-fluoro-10-methyl-19-methyl-20-oxa-3,4,9,10,11,23-hexaazapentacyclo[19.3.1.0 2,6 .0 8,12 .0 13,18 ]pentacosa-1(24),2(6),4,8,11,13,15,17,21(25),22-decaen-22-ylamine.
The chemical structure of zidesamtinib is as follows: Zidesamtinib is a white to tan powder with a pKa of 4.89. The aqueous solubility of zidesamtinib at 37°C is pH dependent, decreasing from 25 mg/mL at pH 2.5 to less than 0.1 mg/mL at pH 7.9. The log of the distribution coefficient (octanol/water) at pH 7.4 is 3.01.
JIDEYTRO (zidesamtinib) tablets for oral use are supplied as 25 mg and 100 mg dosage strengths. JIDEYTRO tablets, 25 mg are film-coated, oblong, pink tablets, debossed with "25" on one side and "ZDS" on the other side of the tablet. JIDEYTRO tablets, 100 mg are film-coated, oblong, yellow tablets, debossed with "100" on one side and "ZDS" on the other side of the tablet.
Inactive ingredients in the tablet core are hydroxypropyl cellulose, magnesium stearate, mannitol, microcrystalline cellulose and sodium starch glycolate. The 25 mg tablet pink film coating contains the inactive ingredients hypromellose, red iron oxide, titanium dioxide, triacetin, and yellow iron oxide. The 100 mg tablet yellow film coating contains the inactive ingredients hypromellose, titanium dioxide, triacetin, and yellow iron oxide.
Zidesamtinib Chemical Structure