Bosutinib 400 mg Tablet, Film Coated, 30-count
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Kinase Inhibitor class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 Clinical
- You have a type of leukemia called Ph+ CML, which is driven by a faulty protein in your blood cells called BCR-ABL. Think of it like a stuck 'on' switch that keeps telling those ce...
- What exactly is bosutinib treating in my body?
- Yes — this is actually pretty important. Food significantly increases how much of the medicine your body absorbs, so taking it on an empty stomach means you'd be getting much less...
- Do I have to take it with food every single time?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Bosutinib — tap one for details:
Where does this data come from?
Ask a licensed pharmacist directly — free, answered by our team.
🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
-
UNII 2S7830E561
Crospovidone is a synthetic polymer derived from povidone. It acts as a disintegrant, helping the tablet or capsule break apart quickly in the stomach so the active ingredient can be absorbed.
-
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.
-
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.
-
UNII 3NXW29V3WO
Hypromellose is a plant-based thickener made from cellulose. It's used in medicines as a binder to hold ingredients together, a coating for tablets, and a thickener for liquids.
-
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.
-
UNII OP1R32D61U
Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
-
UNII LQA7B6G8JG
A synthetic polymer made by combining water-soluble compounds. It acts as a surfactant and solubilizer to help mix oil and water-based ingredients, improving the medicine's texture and how active ingredients dissolve.
-
UNII 3WJQ0SDW1A
Polyethylene glycol is a synthetic liquid or solid polymer used in medicines as a solvent, lubricant, and humectant. It helps dissolve active ingredients, reduces friction during manufacturing, and retains moisture in the final product.
-
UNII K0KQV10C35
Povidone K25 is a synthetic polymer made from vinyl pyrrolidone. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in the stomach for better absorption.
-
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.
10 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
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
Are inactive ingredients the same for every manufacturer?
Why might an inactive ingredient be missing?
Can inactive ingredients matter?
💲 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. | |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Bosulif 400 mg 00069-0193-01 | Pfizer | 30 tablets | — | AB | FDA listed | — |
| Bosulif 400 mg 63539-0193-30 | U.S. | 30 tablets | — | AB | FDA listed | — |
| Bosutinib 400 mgthis 75907-0405-30 | Dr. | 30 tablets | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
Where does this data come from?
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 75907-0405-30 You're viewing this | 30 TABLET, FILM COATED in 1 BOTTLE (75907-405-30) | 2026-06-12 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| 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 | — Not published for this NDC No photo available yet for this listing. |
| 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 | ✓ Available |
| 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. |
Questions about this listing
Why is there no price listed?
Is the NDC printed on the package the same as the 11-digit billing NDC?
What do the three segments of this NDC mean?
Is this package still being marketed?
Who lists this product with the FDA?
Do I need a prescription for this product?
Where does this data come from?
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Bosutinib tablets are indicated for the treatment of: Adult patients with chronic phase (CP) Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML), newly-diagnosed or resistant or intolerant to prior therapy [see Clinical Studies ( 14.1 , 14.2 )] . Adult patients with accelerated phase (AP), or blast phase (BP) Ph+ CML with resistance or intolerance to prior therapy [see Clinical Studies (14.2 )]. Pediatric use information is approved for PF PRISM CV’s BOSULIF ® (bosutinib) tablets.
However, due to PF PRISM CV’s marketing exclusivity rights, this drug product is not labeled with that information. Bosutinib tablets are a kinase inhibitor indicated for the treatment of adult patients with chronic phase Ph+ chronic myelogenous leukemia (CML), newly-diagnosed or resistant or intolerant to prior therapy. ( 1 ) adult patients with accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy.
( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Adult patients with newly-diagnosed chronic phase Ph+ CML: 400 mg orally once daily with food. ( 2.1 ) Adult patients with chronic, accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy: 500 mg orally once daily with food. ( 2.1 ) Consider dose escalation by increments of 100 mg once daily to a maximum of 600 mg daily in adult patients who do not reach complete hematologic, cytogenetic, or molecular response and do not have Grade 3 or greater adverse reactions.
( 2.2 ) Adjust dosage for toxicity and organ impairment ( 2 )
2.1Recommended Dosage The recommended dosage is taken orally once daily with food. Swallow tablets whole. Do not cut, crush, break or chew tablets.
Continue treatment with bosutinib tablets until disease progression or intolerance to therapy. If a dose is missed beyond 12 hours, the patient should skip the dose and take the usual prescribed dose on the following day. Dosage in Adult Patients with Newly-Diagnosed CP Ph+ CML The recommended dosage of bosutinib tablet is 400 mg orally once daily with food.
Dosage in Adult Patients with CP, AP, or BP Ph+ CML with Resistance or Intolerance to Prior Therapy The recommended dosage of bosutinib tablet is 500 mg orally once daily with food. Pediatric use information is approved for PF PRISM CV’s BOSULIF ® (bosutinib) tablets. However, due to PF PRISM CV’s marketing exclusivity rights, this drug product is not labeled with that information .
2.2Dose Escalation In clinical studies of adult patients with Ph+ CML, dose escalation by increments of 100 mg once daily to a maximum of 600 mg once daily was allowed in patients who did not achieve or maintain a hematologic, cytogenetic, or molecular response and who did not have Grade 3 or higher adverse reactions at the recommended starting dosage. The maximum dose in adult patients is 600 mg once daily. Pediatric use information is approved for PF PRISM CV’s BOSULIF ® (bosutinib) tablets.
However, due to PF PRISM CV’s marketing exclusivity rights, this drug product is not labeled with that information.
2.3Dosage Adjustments for Non-Hematologic Adverse Reactions Elevated liver transaminases: If elevations in liver transaminases greater than 5×institutional upper limit of normal (ULN) occur, withhold bosutinib tablets until recovery to less than or equal to 2.5×ULN and resume at 400 mg once daily thereafter. If recovery takes longer than 4 weeks, discontinue bosutinib tablets. If transaminase elevations greater than or equal to 3×ULN occur concurrently with bilirubin elevations greater than 2×ULN and alkaline phosphatase less than 2×ULN (Hy’s law case definition), discontinue bosutinib tablets [see Warnings and Precautions (5.3 )].
Diarrhea: For National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) Grade 3 to 4 diarrhea (increase of greater than or equal to 7 stools/day over baseline/pretreatment), withhold bosutinib tablets until recovery to Grade less than or equal to 1. Bosutinib tablets may be resumed at 400 mg once daily [see Warnings and Precautions (5.1 )] . For other clinically significant, moderate or severe non-hematological toxicity, withhold bosutinib tablets until the toxicity has resolved, then consider resuming bosutinib tablets at a dose reduced by 100 mg taken once daily.
If clinically appropriate, consider re-escalating the dose of bosutinib tablets to the starting dose taken once daily. Pediatric use information is approved for PF PRISM CV’s BOSULIF ® (bosutinib) tablets. However, due to PF PRISM CV’s marketing exclusivity rights, this drug product is not labeled with that information.
2.4Dosage Adjustments for Myelosuppression Dose reductions for severe or persistent neutropenia and thrombocytopenia are described below (Table 3). Table 3: Dose Adjustments for Neutropenia and Thrombocytopenia in Adult Patients ANC a less than 1,000×10 6 /L or Platelets less than 50,000×10 6 /L Withhold bosutinib tablets until ANC great…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS 400 mg: orange, oval, biconvex, film-coated tablets debossed with ''400'' on one side and “B” on other side. Tablets: 400 mg. (3)
⛔ Contraindications ▾
4 CONTRAINDICATIONS Bosutinib tablets are contraindicated in patients with a history of hypersensitivity to bosutinib. Reactions have included anaphylaxis [see Adverse Reactions (6.1 )]. Hypersensitivity to bosutinib. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Gastrointestinal Toxicity: Monitor and manage as necessary. Withhold, dose reduce, or discontinue bosutinib. ( 2.3, 5.1 ) Myelosuppression: Monitor blood counts and manage as necessary.
Withhold, dose reduce, or discontinue bosutinib. ( 2.4 , 5.2 ) Hepatic Toxicity: Monitor liver enzymes at least monthly for the first 3 months and as needed. Withhold, dose reduce, or discontinue bosutinib.
( 2.3, 5.3 ) Cardiovascular Toxicity: Monitor and manage as necessary. Interrupt, dose reduce, or discontinue bosutinib. ( 5.4 ) Fluid Retention: Monitor patients and manage using standard of care treatment.
Interrupt, dose reduce, or discontinue bosutinib. ( 2.3, 5.5 ) Renal Toxicity: Monitor patients for renal function at baseline and during therapy with bosutinib. ( 5.6 ) Embryo-Fetal Toxicity: Bosutinib can cause fetal harm.
Advise female patients of reproductive potential of potential risk to a fetus and to use effective contraception. ( 5.7 )
5.1Gastrointestinal Toxicity Diarrhea, nausea, vomiting, and abdominal pain occur with bosutinib treatment. Monitor and manage patients using standards of care, including antidiarrheals, antiemetics, and fluid replacement. In the randomized clinical trial in adult patients with newly-diagnosed Ph+ CML, the median time to onset for diarrhea (all grades) was 4 days and the median duration per event was 3 days.
Among 546 adult patients in a single-arm study in patients with CML who were resistant or intolerant to prior therapy, the median time to onset for diarrhea (all grades) was 2 days and the median duration per event was 2 days. Among the patients who experienced diarrhea, the median number of episodes of diarrhea per patient during treatment with bosutinib was 3 (range 1 to 268). To manage gastrointestinal toxicity, withhold, dose reduce, or discontinue bosutinib as necessary [see Dosage and Administration (2.3 ) and Adverse Reactions (6 )].
Pediatric use information is approved for PF PRISM CV’s BOSULIF ® (bosutinib) tablets. However, due to PF PRISM CV’s marketing exclusivity rights, this drug product is not labeled with that information.
5.2Myelosuppression Thrombocytopenia, anemia and neutropenia occur with bosutinib treatment. Perform complete blood counts weekly for the first month of therapy and then monthly thereafter, or as clinically indicated. To manage myelosuppression, withhold, dose reduce, or discontinue bosutinib as necessary [see Dosage and Administration (2.4) and Adverse Reactions (6) ].
5.3Hepatic Toxicity Bosutinib may cause elevations in serum transaminases (alanine aminotransferase [ALT], aspartate aminotransferase [AST]). Two cases consistent with drug induced liver injury (defined as concurrent elevations in ALT or AST greater than or equal to 3×ULN with total bilirubin greater than 2×ULN and alkaline phosphatase less than 2×ULN) have occurred without alternative causes. This represented 2 out 1,711 patients in bosutinib clinical trials.
In the 268 adult patients from the safety population in the randomized clinical trial in patients with newly-diagnosed CML in the bosutinib treatment group, the incidence of ALT elevation was 68.3% and increased AST was 56%. Of patients who experienced increased transaminases of any grade, 73% experienced their first increase within the first 3 months. The median time to onset of increased ALT and AST was 29 and 56 days, respectively, and the median duration was 19 and 15 days, respectively.
Among the 546 adult patients in a single-arm study in patients with CML who were resistant or intolerant to prior therapy, the incidence of increased ALT was 53.3% and AST elevation was 46.7%. Sixty percent of the patients experienced an increase in either ALT or AST. Most cases of transaminase elevations in this study occurred early in treatment; of patients who experienced increased transaminases of any grade, more than 81% experienced their first increase within the first 3 months.
The median time to onset of increas…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are discussed in greater detail in other sections of the labeling: • Gastrointestinal toxicity [see Warnings and Precautions (5.1) ]. • Myelosuppression [see Warnings and Precautions (5.2) ]. • Hepatic toxicity [see Warnings and Precautions (5.3 )]. • Cardiovascular toxicity [see Warnings and Precautions (5.4) ]. • Fluid retention [see Warnings and Precautions (5.5) ]. • Renal toxicity [see Warnings and Precautions (5.6) ]. Most common adverse reactions (≥20%), in adult patients with CML are diarrhea, abdominal pain, vomiting, nausea, rash, fatigue, hepatic dysfunction, headache, pyrexia, respiratory tract infection.
The most common laboratory abnormalities (≥20%) in adult patients are creatinine increased, hemoglobin decreased, lymphocyte count decreased, platelets decreased, ALT increased, calcium decreased, white blood cell count decreased, AST increased, absolute neutrophil count decreased, glucose increased, phosphorus decreased, urate increased, alkaline phosphatase increased, lipase increased, creatine kinase increased, and amylase increased. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Dr. Reddy's Laboratories Inc., at 1-888-375-3784 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 most common adverse reactions, in ≥20% of adults with newly diagnosed CP Ph+ CML or CP, AP, or BP Ph+ CML with resistance or intolerance to prior therapy (N=814) were diarrhea (80%), rash (44%), nausea (44%), abdominal pain (43%), vomiting (33%), fatigue (33%), hepatic dysfunction (33%), respiratory tract infection (25%), pyrexia (24%), and headache (21%).
The most common laboratory abnormalities that worsened from baseline in ≥20% of adults were creatinine increased (93%), hemoglobin decreased (90%), lymphocyte count decreased (72%), platelets decreased (69%), ALT increased (58%), calcium decreased (53%), white blood cell count decreased (52%), absolute neutrophils count decreased (50%), AST increased (50%), glucose increased (46%), phosphorus decreased (44%), urate increased (41%), alkaline phosphatase increased (40%), lipase increased (36%), creatine kinase increased (29%), and amylase increased (24%).
Adverse Reactions in Adult Patients With Newly-Diagnosed CP CML The clinical trial randomized and treated 533 patients with newly-diagnosed CP CML to receive bosutinib 400 mg daily or imatinib 400 mg daily as single agents (Newly-Diagnosed CP CML Study) [see Clinical Studies (14.1) ] . The safety population (received at least 1 dose of bosutinib) included: two hundred sixty-eight (268) patients with newly-diagnosed CP CML had a median duration of bosutinib treatment of 55 months (range: 0.3 to 60 months) and a median dose intensity of 394 mg/day.
Serious adverse reactions occurred in 22% of patients with newly-diagnosed CP CML who received bosutinib. Serious adverse reactions reported in >2% of patients included hepatic dysfunction (4.1%), pneumonia (3.4%), coronary artery disease (3.4%), and gastroenteritis (2.2%). Fatal adverse reactions occurred in 3 patients (1.1%) due to coronary artery disease (0.4%), cardiac failure acute (0.4%), and renal failure (0.4%).
Permanent discontinuation of bosutinib due to an adverse reaction occurred in 20% of patients with newly-diagnosed CP CML who received bosutinib. Adverse reactions which resulted in permanent discontinuation in > 2% of patients included hepatic dysfunction (9%). Dose modifications (dose interruption or reductions) of bosutinib due to an adverse reaction occurred in 68% of patients with newly-diagnosed CP CML.
Adverse reactions which required dose interruptions or reductions in >5% of patients included hep…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS • Strong and Moderate CYP3A Inhibitors: Avoid concomitant use with bosutinib. ( 7.1 ) • Strong CYP3A Inducers: Avoid concomitant use with bosutinib. ( 7.1 ) • Proton Pump Inhibitors: Use short-acting antacids or H2 blockers as an alternative to proton pump inhibitors. ( 7.1 )
7.1Effect of Other Drugs on Bosutinib Strong or Moderate CYP3A Inhibitors Avoid the concomitant use of strong or moderate CYP3A inhibitors with bosutinib. Bosutinib is a CYP3A substrate. Concomitant use with a strong or moderate CYP3A inhibitor increases bosutinib C max and AUC [see Clinical Pharmacology (12.3) ] which may increase the risk of toxicities.
Strong CYP3A Inducers Avoid the concomitant use of strong CYP3A inducers with bosutinib. Bosutinib is a CYP3A substrate. Concomitant use with a strong CYP3A inducer decreases bosutinib C max and AUC [see Clinical Pharmacology (12.3 )] which may reduce bosutinib efficacy.
Proton Pump Inhibitors (PPI) As an alternative to PPIs, use short-acting antacids or H2 blockers and separate dosing by more than 2 hours from bosutinib dosing. Bosutinib displays pH dependent aqueous solubility, Concomitant use with a PPI decreases bosutinib C max and AUC [see Clinical Pharmacology (12.3 )] which may reduce bosutinib efficacy.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Lactation: Advise women not to breastfeed. ( 8.2 ) Pediatric use information is approved for PF PRISM CV’s BOSULIF ® (bosutinib) tablets. However, due to PF PRISM CV’s marketing exclusivity rights, this drug product is not labeled with that information.
8.1Pregnancy R isk Summary Based on findings from animal studies and its mechanism of action, bosutinib can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ]. There are no available data in pregnant women to inform the drug-associated risk. In animal reproduction studies conducted in rats and rabbits, oral administration of bosutinib during organogenesis caused adverse developmental outcomes, including structural abnormalities, embryo-fetal mortality, and alterations to growth at maternal exposures (AUC) as low as 1.2 times the human exposure at the dose of 500 mg/day ( see Data ).
Advise pregnant women of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies are 2 to 4% and 15 to 20%, respectively. D ata A nimal Data In a rat fertility and early embryonic development study, bosutinib was administered orally to female rats for approximately 3 to 6 weeks, depending on day of mating (2 weeks prior to cohabitation with untreated breeder males until gestation day [GD] 7). Increased embryonic resorptions occurred at greater than or equal to 10 mg/kg/day of bosutinib (1.6 and 1.2 times the human exposure at the recommended doses of 400 or 500 mg/day, respectively), and decreased implantations and reduced number of viable embryos at 30 mg/kg/day of bosutinib (3.4 and 2.5 times the human exposure at the recommended doses of 400 or 500 mg/day, respectively).
In an embryo-fetal development study conducted in rabbits, bosutinib was administered orally to pregnant animals during the period of organogenesis at doses of 3, 10, and 30 mg/kg/day. At the maternally-toxic dose of 30 mg/kg/day of bosutinib, there were fetal anomalies (fused sternebrae, and 2 fetuses had various visceral observations), and an approximate 6% decrease in fetal body weight. The dose of 30 mg/kg/day resulted in exposures (AUC) approximately 5.1 and 3.8 times the human exposures at the recommended doses of 400 and 500 mg/day, respectively.
Fetal exposure to bosutinib-derived radioactivity during pregnancy was demonstrated in a placental-transfer study in pregnant rats. In a rat pre- and postnatal development study, bosutinib was administered orally to pregnant animals during the period of organogenesis through lactation day 20 at doses of 10, 30, and 70 mg/kg/day. Reduced number of pups born occurred at greater than or equal to 30 mg/kg/day bosutinib (3.4 and 2.5 times the human exposure at the recommended doses of 400 or 500 mg/day, respectively), and increased incidence of total litter loss and decreased growth of offspring after birth occurred at 70 mg/kg/day bosutinib (6.9 and 5.1 times the human exposure at the recommended doses of 400 or 500 mg/day, respectively).
8.2Lactation Risk Summary No data are available regarding the presence of bosutinib or its metabolites in human milk or its effects on a breastfed child or on milk production. However, bosutinib is present in the milk of lactating rats. Because of the potential for serious adverse reactions in a nursing child, breastfeeding is not recommended during treatment with bosutinib and for 2 weeks after the last dose.
Animal Data After a single radiolabeled bosutinib dose to lactating rats, radioactivity was present in the plasma of suckling offspring for 24 to 48 hours.
8.3Females and Males of Reproductive Potential Based on findings from animal studies, bosutinib can cause fetal harm when…
🤰 Pregnancy ▾
8.1Pregnancy R isk Summary Based on findings from animal studies and its mechanism of action, bosutinib can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ]. There are no available data in pregnant women to inform the drug-associated risk. In animal reproduction studies conducted in rats and rabbits, oral administration of bosutinib during organogenesis caused adverse developmental outcomes, including structural abnormalities, embryo-fetal mortality, and alterations to growth at maternal exposures (AUC) as low as 1.2 times the human exposure at the dose of 500 mg/day ( see Data ).
Advise pregnant women of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies are 2 to 4% and 15 to 20%, respectively. D ata A nimal Data In a rat fertility and early embryonic development study, bosutinib was administered orally to female rats for approximately 3 to 6 weeks, depending on day of mating (2 weeks prior to cohabitation with untreated breeder males until gestation day [GD] 7). Increased embryonic resorptions occurred at greater than or equal to 10 mg/kg/day of bosutinib (1.6 and 1.2 times the human exposure at the recommended doses of 400 or 500 mg/day, respectively), and decreased implantations and reduced number of viable embryos at 30 mg/kg/day of bosutinib (3.4 and 2.5 times the human exposure at the recommended doses of 400 or 500 mg/day, respectively).
In an embryo-fetal development study conducted in rabbits, bosutinib was administered orally to pregnant animals during the period of organogenesis at doses of 3, 10, and 30 mg/kg/day. At the maternally-toxic dose of 30 mg/kg/day of bosutinib, there were fetal anomalies (fused sternebrae, and 2 fetuses had various visceral observations), and an approximate 6% decrease in fetal body weight. The dose of 30 mg/kg/day resulted in exposures (AUC) approximately 5.1 and 3.8 times the human exposures at the recommended doses of 400 and 500 mg/day, respectively.
Fetal exposure to bosutinib-derived radioactivity during pregnancy was demonstrated in a placental-transfer study in pregnant rats. In a rat pre- and postnatal development study, bosutinib was administered orally to pregnant animals during the period of organogenesis through lactation day 20 at doses of 10, 30, and 70 mg/kg/day. Reduced number of pups born occurred at greater than or equal to 30 mg/kg/day bosutinib (3.4 and 2.5 times the human exposure at the recommended doses of 400 or 500 mg/day, respectively), and increased incidence of total litter loss and decreased growth of offspring after birth occurred at 70 mg/kg/day bosutinib (6.9 and 5.1 times the human exposure at the recommended doses of 400 or 500 mg/day, respectively).
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of bosutinib in pediatric patients younger than 1 year of age with newly diagnosed CP Ph+ CML, pediatric patients younger than 1 year of age with CP Ph+ CML that is resistant or intolerant to prior therapy, and pediatric patients with AP Ph+ CML or BP Ph+ CML have not been established. Pediatric use information is approved for PF PRISM CV’s BOSULIF® (bosutinib) tablets. However, due to PF PRISM CV’s marketing exclusivity rights, this drug product is not labeled with that information.
🧓 Geriatric Use ▾
8.5Geriatric Use In the single-arm study in patients with CML who were resistant or intolerant to prior therapy of bosutinib in patients with Ph+ CML, 20% were age 65 and over, 4% were 75 and over. Of the 268 patients who received bosutinib in the study for newly diagnosed CML, 20% were age 65 and over, 5% were 75 and over. No overall differences in safety or effectiveness were observed between these patients and younger patients, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
🆘 Overdosage ▾
10 OVERDOSAGE Experience with bosutinib overdose in clinical studies was limited to isolated cases. There were no reports of any serious adverse events associated with the overdoses. Patients who take an overdose of bosutinib should be observed and given appropriate supportive treatment.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Bosutinib is a TKI. Bosutinib inhibits the BCR-ABL kinase that promotes CML; it is also an inhibitor of Src-family kinases including Src, Lyn, and Hck. Bosutinib inhibited 16 of 18 imatinib-resistant forms of BCR-ABL kinase expressed in murine myeloid cell lines. Bosutinib did not inhibit the T315I and V299L mutant cells.
12.2Pharmacodynamics A greater likelihood of response and a greater likelihood of safety events were observed with higher bosutinib exposure in clinical studies. The time course of bosutinib pharmacodynamic response has not been fully characterized. Cardiac Electrophysiology At a single oral dose of 500 mg bosutinib with ketoconazole (a strong CYP3A inhibitor), bosutinib does not prolong the QT interval to any clinically relevant extent.
12.3Pharmacokinetics Bosutinib pharmacokinetics were assessed following oral dosing with food in adult patients with CML and were presented as geometric mean (CV%), unless otherwise specified. Bosutinib exhibits dose proportional increases in C max and AUC over the oral dose range of 200 to 800 mg (0.33 to 1.3 times the maximum approved recommended dosage of 600 mg). Bosutinib steady state C max was 127 ng/mL (31%), C trough was 68 ng/mL (39%) and AUC was 2,370 ng•h/mL (34%) following multiple oral doses of bosutinib 400 mg; Bosutinib steady state C max was 171 ng/mL (38%), C trough was 91 ng/mL (42%) and AUC was 3,150 ng•h/mL (38%) following multiple oral doses of bosutinib 500 mg.
No clinically significant differences in the pharmacokinetics of bosutinib were observed following administration of either the tablet dosage forms of bosutinib at the same dose, under fed conditions. Absorption The median bosutinib (minimum, maximum) time--to-C max (t max ) was 6 (6, 6) hours following oral administration of a single oral dose of bosutinib 500 mg with food. The absolute bioavailability was 34% in healthy subjects.
Effect of Food Bosutinib C max increased 1.8-fold and AUC increased 1.7-fold when bosutinib tablets were given with a high fat meal to healthy subjects compared to administration under fasted condition. Bosutinib C max increased 1.6-fold and AUC increased 1.5-fold when bosutinib capsules were given with a high fat meal to healthy subjects compared to administration under fasted condition. The high-fat meal (800 to 1,000 total calories) consisted of approximately 150 protein calories, 250 carbohydrate calories, and 500 to 600 fat calories.
No clinically significant differences in the pharmacokinetics of bosutinib were observed following administration of a bosutinib capsule that was opened and the contents mixed with applesauce or yogurt immediately before use. Distribution The mean (SD) apparent bosutinib volume of distribution is 6,080 (1,230) L after an oral dose of 500 mg of bosutinib. Bosutinib protein binding is 94% in vitro and 96% ex vivo, and is independent of concentration.
Elimination The mean (SD) bosutinib terminal phase elimination half life (t ½ ) was 22.5 (1.7) hours, and the mean (SD) apparent clearance was 189 (48) L/h following a single oral dose of bosutinib. Metabolism Bosutinib is primarily metabolized by CYP3A4. Excretion Following a single oral dose of [ 14 C] radiolabeled bosutinib without food, 91.3% of the dose was recovered in feces and 3.3% of the dose recovered in urine.
Specific Populations Patients with Renal Impairment Bosutinib AUC increased 1.4-fold in subjects with moderate renal impairment (CL cr : 30 to 50 mL/min, estimated by Cockcroft-Gault (C-G)) and increased 1.6-fold in subjects with severe renal impairment (CL cr less than 30 mL/min) following a single oral dose of bosutinib 200 mg (0.33 times the maximum approved recommended dosage of 600 mg). No clinically significant difference in the pharmacokinetics of bosutinib was observed in subjects with mild renal impairment (CL cr : 51 to 80 mL/min, C-G) .
Bosutinib has not been studied in patients undergoing hemodialysis. Patients…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Bosutinib is a TKI. Bosutinib inhibits the BCR-ABL kinase that promotes CML; it is also an inhibitor of Src-family kinases including Src, Lyn, and Hck. Bosutinib inhibited 16 of 18 imatinib-resistant forms of BCR-ABL kinase expressed in murine myeloid cell lines. Bosutinib did not inhibit the T315I and V299L mutant cells.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Tablets - How Supplied Bosutinib tablets are supplied for oral administration in a single strength 400 mg orange, oval, biconvex, film-coated tablets debossed with “400” on one side and “B” on other side. Bosutinib tablets are available in the following packaging configurations with a child-resistant CR) closure (Table 17). Bottles contain a desiccant.
Table 17: Tablet Presentations Bosutinib Tablets Package Configuration Tablet Strength (mg) NDC Tablet Description 30 tablets per bottle 400 mg 75907-405-30 Orange, oval, biconvex, film-coated tablets, debossed with “400” on one side and “B” on other side. Abbreviation: NDC=National drug code. Storage Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].
Handling and Disposal Procedures for proper disposal of anticancer drugs should be considered. Touching or handling crushed or broken tablets is to be avoided. Any unused product or waste material should be disposed of in accordance with local requirements, or drug take back programs.
📋 Description ▾
11 DESCRIPTION Bosutinib tablets contains bosutinib, a kinase inhibitor. The chemical name of bosutinib is 3-Quinolinecarbonitrile, 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl) propoxy]-hydrate (1:2). Its chemical formula is C 26 H 29 Cl 2 N 5 O 3 .2H 2 O; its molecular weight is 566.48 Bosutinib has the following chemical structure: Bosutinib is a white to yellowish-tan powder.
Bosutinib is soluble in dimethyl sulfoxide, sparingly soluble in acetone and practically insoluble in water. Bosutinib tablets are supplied for oral administration in a single strength of 400 mg, equivalent to 400 mg of bosutinib on an anhydrous basis. The tablets contain the following inactive ingredients: crospovidone, hypromellose, magnesium stearate, microcrystalline cellulose, poloxamer, povidone, titanium dioxide, polyethylene glycol, iron oxide yellow and iron oxide red. bosutinib-structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information and Instructions for Use). • Dosage and Administration Instruct patients to take bosutinib exactly as prescribed, not to change their dose or to stop taking bosutinib unless they are told to do so by their doctor. If patients miss a dose beyond 12 hours, they should be advised to take the next scheduled dose at its regular time. A double dose should not be taken to make up for any missed dose.
Advise patients to take bosutinib with food. Patients should be advised: “Swallow tablets whole. Do not crush, break, or cut tablet.
Do not touch or handle crushed or broken tablets." • Gastrointestinal Toxicity Advise patients that they may experience diarrhea, nausea, vomiting, abdominal pain, or blood in their stools with bosutinib and to seek medical attention promptly for these symptoms [see Warnings and Precautions (5.1)]. • Myelosuppression Advise patients of the possibility of developing low blood cell counts and to immediately report fever, any suggestion of infection, or signs or symptoms suggestive of bleeding or easy bruising [see Warnings and Precautions (5.2) ]. • Hepatic Toxicity Advise patients of the possibility of developing liver function abnormalities and to immediately report jaundice [see Warnings and Precautions (5.3) ]. • Cardiovascular Toxicity Advise patients that cardiac failure, left ventricular dysfunction, and cardiac ischemic events have been reported.
Advise patients to seek immediate medical attention if any symptoms suggestive of cardiac failure and cardiac ischemia occur, such as shortness of breath, weight gain, or fluid retention [see Warnings and Precautions (5.4) ]. • Fluid Retention Advise patients of the possibility of developing fluid retention (swelling, weight gain, or shortness of breath) and to seek medical attention promptly if these symptoms arise [see Warnings and Precautions (5.5) ]. • Renal Toxicity Advise patients of the possibility of developing renal problems and to immediately report frequent urination, polyuria or oliguria [see Warnings and Precautions (5.6) ]. • Adverse Reactions Advise patients that they may experience other adverse reactions such as respiratory tract infections, rash, fatigue, headache, dizziness, back pain, arthralgia, pruritus with bosutinib and to seek medical attention if symptoms are significant.
There is a possibility of anaphylactic shock [see Contraindications (4 ) and Adverse Reactions (6 )]. • Embryo-Fetal Toxicity Advise females to inform their healthcare provider if they are pregnant or become pregnant. Advise female patients of the risk to a fetus and potential loss of the pregnancy [see Use in Specific Populations (8.1) ]. Advise females of reproductive potential, to use effective contraception during treatment and for 2 weeks after receiving the last dose of bosutinib [see Warnings and Precautions (5.7) and Use in Specific Populations (8.1 , 8.3) ].
Advise lactating women not to breastfeed during treatment with bosutinib and for 2 weeks after the last dose [see Use in Specific Populations (8.2) ]. • Drug Interactions Advise patients that bosutinib and certain other medicines, including over the counter medications or herbal supplements (such as St. John’s wort) can interact with each other and may alter the effects of bosutinib [see Drug Interactions (7) ]. Manufactured by: MSN Laboratories Private Limited Telangana – 509 228, INDIA Distributor Dr.
Reddy's Laboratories Inc., Princeton, NJ 08540 Made in India Issued: 04/2026