QINLOCK Ripretinib 50 mg Tablet, 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
Ripretinib is used to treat gastrointestinal stromal tumors (GIST; a type of tumor that grows in the stomach, intestine [bowel], or esophagus [tube that connects the throat with the stomach]) in adults who have previously received other medications, including imatinib (Gleevec). Ripretinib is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps slow or stop the spread of cancer cells.
Read the full MedlinePlus article ↗- Qinlock is prescribed for a type of digestive-tract cancer called gastrointestinal stromal tumor, or GIST. Specifically, it's for patients who have already tried at least three oth...
- What exactly is Qinlock used for, and why was I prescribed it?
- No, it doesn't — you can take Qinlock with or without food, whichever is easier for you. What does matter is taking it at the same time every day. Swallow the tablet whole and don'...
- Does it matter if I take Qinlock with food or on an empty stomach?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Ripretinib — tap one for details:
Where does this data come from?
Ask a licensed pharmacist directly — free, answered by our team.
💊 What it looks like
Where does this data come from?
🧪 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.
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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.
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UNII 6N003M473W
Hypromellose acetate succinate is a modified cellulose polymer that dissolves in the small intestine. It's used as a coating material to protect the medicine from stomach acid and control where and when the drug is released in the digestive tract.
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UNII EWQ57Q8I5X
Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
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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 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.
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UNII ETJ7Z6XBU4
Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
6 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
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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 · Q2 2026 | $515.00 | $15,449.87 / 30 tablets |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Qinlock 50 mgthis 73207-0101-31 | Deciphera | 30 tablets | — | — | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.
Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.
🛈 What do these terms mean?
- Patent
- Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
- Substance patent
- Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
- Formulation (product) patent
- Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
- Method-of-use patent
- A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
- Skinny label
- A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
- Exclusivity
- FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
- Paragraph IV
- A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
- RLD / RS
- Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
- TE / AB rating
- FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
- LOE (loss of exclusivity)
- The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.
Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.
| Patent | Type | Use code | Expires |
|---|---|---|---|
| US 11426390 ↗ | Method of use | U-3416 | Aug 12, 2040 |
| US 12295944 ↗ | Method of use | U-4183 | Aug 12, 2040 |
| US 11433056 ↗ | Method of use | U-3423 | Aug 12, 2040 |
| US 12023328 ↗ | Method of use | U-3957 | Dec 30, 2040 |
| US 12023327 ↗ | Method of use | U-3958 | Aug 12, 2040 |
| US 12023326 ↗ | Method of use | U-3959 | Aug 12, 2040 |
| US 12023325 ↗ | Method of use | U-3960 | Aug 12, 2040 |
| US 11529336 ↗ | Method of use | U-3382 | Aug 12, 2040 |
| US 11534432 ↗ | Method of use | U-3442 | Aug 12, 2040 |
| US 11969415 ↗ | Method of use | U-3219 | Dec 30, 2040 |
| US 11969414 ↗ | Method of use | U-3897 | Feb 8, 2041 |
| US 12318373 ↗ | Method of use | U-4191 | Aug 12, 2040 |
| US 11779572 ↗ | Method of use | U-3714 | Oct 6, 2042 |
| US 11813251 ↗ | Method of use | U-3750 | Aug 12, 2040 |
| US 11344536 ↗ | Method of use | U-3381 | Aug 12, 2040 |
| US 11266635 ↗ | Method of use | U-3330 | Aug 12, 2040 |
| US 11576904 ↗ | Method of use | U-3537 | Aug 12, 2040 |
| US 12064422 ↗ | Method of use | U-3219 | Dec 30, 2040 |
| US 10966966 ↗ | Method of use | U-3153 | Aug 12, 2040 |
| US 11801237 ↗ | Method of use | U-3219 | Dec 30, 2040 |
| US RE48731 ↗ | Method of use | U-3219 | Jun 7, 2032 |
| US 12059411 ↗ | Method of use | U-3971 | Aug 12, 2040 |
| US 12059410 ↗ | Method of use | U-3153 | Aug 12, 2040 |
| US 11918564 ↗ | Drug product | — | Dec 30, 2040 |
| US 12213967 ↗ | Drug product | — | Dec 30, 2040 |
| US 11896585 ↗ | Drug product | — | Dec 30, 2040 |
| US 12318374 ↗ | Drug product | — | Dec 30, 2040 |
| US 11576903 ↗ | Drug product | — | Dec 30, 2040 |
| US 11903933 ↗ | Drug product | — | Dec 30, 2040 |
| US 12226406 ↗ | Drug product | — | Dec 30, 2040 |
| US 11844788 ↗ | Drug product | — | Dec 30, 2040 |
| US 8188113 ↗ | Drug substance | — | Jul 27, 2030 |
| US 8461179 ↗ | Drug substance | — | May 15, 2034 |
| US 11850241 ↗ | Drug product | — | Dec 30, 2040 |
| US 11395818 ↗ | Drug product | — | Dec 30, 2040 |
| US 11612591 ↗ | Drug product | — | Dec 30, 2040 |
| US 11185535 ↗ | Drug product | — | Dec 30, 2040 |
| US 11793795 ↗ | Drug product | — | Dec 30, 2040 |
| US 12213968 ↗ | Drug product | — | Dec 30, 2040 |
| US 11850240 ↗ | Drug product | — | Dec 30, 2040 |
| US 11911370 ↗ | Drug product | — | Dec 30, 2040 |
| Code | What it grants | Expires |
|---|---|---|
| ODE-298 | Orphan Drug Exclusivity (7-year) | May 15, 2027 |
Is there a generic version of QINLOCK 50 MG TABLET?
The FDA approved a generic — why can’t I get it at my pharmacy yet?
Why do different websites show different generic release dates?
What does “FDA listed” mean?
What does a patent or protection date mean here?
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Can a generic come out before the last patent expires?
Can a generic come out after the listed dates?
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Where does this data come from?
💊 Medicaid utilization by pack size
📊 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 |
|---|---|---|---|
| 73207-0101-30 | 1 BOTTLE in 1 CARTON (73207-101-30) / 90 TABLET in 1 BOTTLE | 2020-05-15 | Active |
| 73207-0101-31 You're viewing this | 1 BOTTLE in 1 CARTON (73207-101-31) / 30 TABLET in 1 BOTTLE | 2020-05-15 | Active |
This pack shows little to no recent Medicaid volume — a different pack size carries most fills. See all packs ↓
Pack size FAQ
What quantity is in NDC 73207-0101-31?
What is the difference between NDC 73207-0101-31 and NDC 73207-0101-30?
What NDC number is used to bill for this package of QINLOCK Ripretinib 50 mg Tablet?
🧭 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 | ✓ 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 | ✓ 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?
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Do I need a prescription for this product?
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE QINLOCK is indicated for the treatment of adult patients with advanced gastrointestinal stromal tumor (GIST) who have received prior treatment with 3 or more kinase inhibitors, including imatinib. QINLOCK is a kinase inhibitor indicated for the treatment of adult patients with advanced gastrointestinal stromal tumor (GIST) who have received prior treatment with 3 or more kinase inhibitors, including imatinib. ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Recommended Dosage : 150 mg orally once daily with or without food. ( 2.1 )
2.1Recommended Dosage The recommended dosage of QINLOCK is 150 mg orally once daily with or without food until disease progression or unacceptable toxicity. Instruct patients to swallow tablets whole. Advise patients to take QINLOCK at the same time each day.
Advise patients to take a missed dose if less than 8 hours have passed since the missed scheduled dose. Advise patients not to take an additional dose if vomiting occurs after taking QINLOCK and to continue with their next scheduled dose.
2.2Dosage Modifications for Adverse Reactions The recommended dose reduction for adverse reactions is: QINLOCK 100 mg orally once daily. Permanently discontinue QINLOCK in patients who are unable to tolerate 100 mg orally once daily. The recommended dosage modifications of QINLOCK for adverse reactions are provided in Table 1 .
Table 1: Recommended Dosage Modifications for QINLOCK for Adverse Reactions Adverse Reaction Severity a QINLOCK Dosage Modifications a Graded per National Cancer Institute Common Terminology Criteria for Adverse Events version 4.03 (NCI CTCAE v4.03). Palmar-Plantar Erythrodysesthesia Syndrome (PPES) [see Warnings and Precautions ( 5.1 )] Grade 2 Withhold QINLOCK until Grade ≤1 or baseline. If recovered within 7 days, resume QINLOCK at same dose; otherwise resume at reduced dose.
Consider re-escalating QINLOCK if maintained at Grade ≤1 or baseline for at least 28 days. If PPES recurs, withhold QINLOCK until Grade ≤1 or baseline and then resume QINLOCK at a reduced dose regardless of time to improvement. Grade 3 Withhold QINLOCK for at least 7 days or until Grade ≤1 or baseline (maximum 28 days).
Resume QINLOCK at a reduced dose. Consider re-escalating QINLOCK if maintained at Grade ≤1 or baseline for at least 28 days. Hypertension [see Warnings and Precautions ( 5.3 )] Grade 3 If symptomatic, withhold QINLOCK until symptoms have resolved and blood pressure is controlled.
If blood pressure is controlled to Grade ≤1 or baseline, resume QINLOCK at the same dose; otherwise, resume QINLOCK at reduced dose. If Grade 3 hypertension recurs, withhold QINLOCK until symptoms have resolved and blood pressure is controlled. Resume QINLOCK at a reduced dose.
Grade 4 Permanently discontinue QINLOCK. Left Ventricular Systolic Dysfunction [see Warnings and Precautions ( 5.4 )] Grade 3 or 4 Permanently discontinue QINLOCK. Arthralgia or Myalgia [see Adverse Reactions ( 6.1 )] Grade 2 Withhold QINLOCK until Grade ≤1 or baseline.
If recovered within 7 days, resume QINLOCK at same dose; otherwise resume QINLOCK at reduced dose. Consider re-escalating QINLOCK if maintained at Grade ≤1 or baseline for at least 28 days. If arthralgia or myalgia recurs, withhold QINLOCK until Grade ≤1 or baseline and then resume QINLOCK at a reduced dose regardless of time to improvement.
Grade 3 Withhold QINLOCK for at least 7 days or until Grade ≤1 or baseline (maximum of 28 days). Resume QINLOCK at a reduced dose. Consider re-escalating QINLOCK if maintained at Grade ≤1 or baseline for at least 28 days.
Other Adverse Reactions [see Adverse Reactions ( 6.1 )] Grade 3 or 4 Withhold QINLOCK until Grade ≤1 or baseline (maximum 28 days), and then resume QINLOCK at a reduced dose; otherwise permanently discontinue. Consider re-escalating QINLOCK if no recurrence of the adverse reaction for at least 28 days. If Grade 3 or 4 recurs, permanently discontinue QINLOCK.
2.3Dose Modifications for Moderate CYP3A Inducers Avoid concomitant use of moderate CYP3A inducers during QINLOCK treatment. If a moderate CYP3A inducer cannot be avoided, increase the QINLOCK dosing frequency from the recommended dose of 150 mg once daily to 150 mg twice daily during the co-administration period. Monitor for clinical response and tolerability.
If the concomitant moderate CYP3A inducer is discontinued, resume QINLOCK dosage back to 150 mg once daily 14 days after the discontinua…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Tablets: 50 mg, white to off-white, oval shaped, debossed with “DC1” on one side. Tablets: 50 mg. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Palmar-Plantar Erythrodysesthesia Syndrome : Based on severity, withhold QINLOCK and resume at same or reduced dose. ( 2.2 , 5.1 ) New Primary Cutaneous Malignancies : Perform dermatologic evaluations when initiating QINLOCK and routinely during treatment. ( 5.2 ) Hypertension : Do not initiate QINLOCK in patients with uncontrolled hypertension and monitor blood pressure during treatment.
Based on severity, withhold QINLOCK and then resume at same or reduced dose or permanently discontinue. ( 2.2 , 5.3 ) Cardiac Dysfunction : Assess ejection fraction by echocardiogram or MUGA scan prior to initiating QINLOCK and during treatment, as clinically indicated. Permanently discontinue QINLOCK for Grade 3 or 4 left ventricular systolic dysfunction.
( 2.2 , 5.4 ) Risk of Impaired Wound Healing : Withhold QINLOCK for at least 1 week prior to elective surgery. Do not administer for at least 2 weeks after major surgery and until adequate wound healing. The safety of resumption of QINLOCK after resolution of wound healing complications has not been established.
( 5.5 ) Photosensitivity : May cause photosensitivity reactions. Advise patients to limit direct ultraviolet exposure. ( 5.6 ) Embryo-Fetal Toxicity : Can cause fetal harm.
Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception. ( 5.7 , 8.1 , 8.3 )
5.1Palmar-Plantar Erythrodysesthesia Syndrome In INVICTUS, Grade 1-2 palmar-plantar erythrodysesthesia syndrome (PPES) occurred in 21% of the 85 patients who received QINLOCK [see Adverse Reactions ( 6.1 )]. PPES led to dose discontinuation in 1.2% of patients, dose interruption in 2.4% of patients, and dose reduction in 1.2% of patients. Based on severity, withhold QINLOCK and then resume at same or reduced dose [see Dosage and Administration ( 2.2 )] .
5.2New Primary Cutaneous Malignancies In INVICTUS, cutaneous squamous cell carcinoma (cuSCC) occurred in 4.7% of the 85 patients who received QINLOCK, with a median time to event of 4.6 months (range: 3.8 to 6 months). In the pooled safety population, cuSCC and keratoacanthoma occurred in 7% and 1.9% of patients, respectively. In INVICTUS, melanoma occurred in 2.4% of the 85 of patients who received QINLOCK.
In the pooled safety population, melanoma occurred in 0.9% of patients. Perform dermatologic evaluations when initiating QINLOCK and routinely during treatment. Manage suspicious skin lesions with excision and dermatopathologic evaluation.
Continue QINLOCK at the same dose.
5.3Hypertension In INVICTUS, Grade 1-3 hypertension occurred in 14% of the 85 patients who received QINLOCK, including Grade 3 hypertension in 7% [see Adverse Reactions ( 6.1 )] . Do not initiate QINLOCK in patients with uncontrolled hypertension. Adequately control blood pressure prior to initiating QINLOCK.
Monitor blood pressure as clinically indicated during treatment with QINLOCK, and initiate or adjust antihypertensive therapy as appropriate. Based on severity, withhold QINLOCK and then resume at same or reduced dose or permanently discontinue [see Dosage and Administration ( 2.2 )] .
5.4Cardiac Dysfunction In INVICTUS, cardiac failure occurred in 1.2% of the 85 patients who received QINLOCK. In the pooled safety population, cardiac dysfunction (including cardiac failure, acute left ventricular failure, diastolic dysfunction, and ventricular hypertrophy) occurred in 1.7% of patients, including Grade 3 adverse reactions in 1.1%. In INVICTUS, Grade 3 decreased ejection fraction occurred in 1.3% of the 77 patients who received QINLOCK and who had a baseline and at least one post-baseline echocardiogram.
In the pooled safety population, Grade 3 decreased ejection fraction occurred in 1.9% of the 263 patients who received QINLOCK and who had a baseline and at least one post-baseline echocardiogram. In INVICTUS, cardiac dysfunction led to dose discontinuation in 1.2% of the 85 patients who received QINLOCK. The safety of QINLOCK ha…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are discussed elsewhere in the labeling: Palmar-Plantar Erythrodysesthesia Syndrome [see Warnings and Precautions ( 5.1 )] New Primary Cutaneous Malignancies [see Warnings and Precautions ( 5.2 )] Hypertension [see Warnings and Precautions ( 5.3 )] Cardiac Dysfunction [see Warnings and Precautions ( 5.4 )] Photosensitivity [see Warnings and Precautions ( 5.6 )] The most common adverse reactions (≥20%) were alopecia, fatigue, nausea, abdominal pain, constipation, myalgia, diarrhea, decreased appetite, palmar-plantar erythrodysesthesia, and vomiting.
The most common Grade 3 or 4 laboratory abnormalities (≥4%) were increased lipase and decreased phosphate. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Deciphera Pharmaceuticals, LLC, at 1-888-724-3274 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. Unless otherwise specified, the pooled safety population described in the WARNINGS AND PRECAUTIONS reflect exposure to QINLOCK as a single agent in 351 patients with advanced solid tumors enrolled in either an open-label dose finding with cohort expansion trial or INVICTUS.
Among the patients who received QINLOCK in these trials, 52% were exposed for 6 months or longer and 21% were exposed for greater than one year. Gastrointestinal Stromal Tumor Patients Who Received Prior Treatment with Imatinib, Sunitinib and Regorafenib The safety of QINLOCK was evaluated in INVICTUS [see Clinical Studies ( 14 )] . Patients received QINLOCK 150 mg taken orally once daily (n=85) or placebo (n=43).
Among the patients who received QINLOCK, 46% were exposed for 6 months or longer and 3.5% were exposed for greater than one year. Serious adverse reactions occurred in 31% of patients who received QINLOCK. Serious adverse reactions that occurred in >2% of patients were abdominal pain (4.7%), anemia (3.5%), nausea (2.4%), and vomiting (2.4%).
Permanent discontinuation due to an adverse reaction occurred in 8% of patients who received QINLOCK. Adverse reactions resulting in permanent discontinuation in ≥1% of patients included general physical health deterioration (2.4%), anemia (1.2%), cardiac failure (1.2%), PPES (1.2%), and vomiting (1.2%). Dosage interruptions due to an adverse reaction occurred in 24% of patients who received QINLOCK.
Adverse reactions requiring dosage interruption in >2% of patients included nausea (3.5%), increased blood bilirubin (2.4%), and PPES (2.4%). Dose reductions due to an adverse reaction occurred in 7% of patients who received QINLOCK. Adverse reactions resulting in a dose reduction in ≥1.2% of patients were abdominal pain, agitation, alopecia, arthritis, dermatosis, gastrointestinal disorder, hyperesthesia, myalgia, PPES, and decreased weight.
The most common adverse reactions (≥20%), were alopecia, fatigue, nausea, abdominal pain, constipation, myalgia, diarrhea, decreased appetite, PPES, and vomiting. The most common Grade 3 or 4 laboratory abnormalities (≥4%) were increased lipase and decreased phosphate. Table 2 summarizes the adverse reactions in INVICTUS.
Table 2: Adverse Reactions (≥10%) in Patients with Gastrointestinal Stromal Tumor Who Received QINLOCK in INVICTUS Adverse Reaction QINLOCK (N=85) Placebo (N=43) Grades 1-4 Grades 3-4 Grades 1-4 Grades 3-4 Skin and subcutaneous tissue Alopecia 52 0 4.7 0 Palmar-plantar erythrodysesthesia syndrome 21 0 0 0 Dry skin 13 0 7 0 Pruritus 11 0 4.7 0 General Fatigue 42 3.5 23
2.3Peripheral edema 17 1.2 7 0 Asthenia 13 1.2 14
4.7Gastrointestinal Nausea 39 3.5 12 0 Abdominal pain 36 7 30
4.7Constipation 34 1.2 19 0 Diarrhea 28 1.2 14
2.3Vomiting 21 3.5 7 0 Stomatitis 11 0 0 0 Musculoskeletal and conn…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Strong CYP3A Inhibitors : Monitor more frequently for adverse reactions. ( 7.1 ) Strong CYP3A Inducers : Avoid concomitant use of strong CYP3A inducers. ( 7.1 ) Moderate CYP3A Inducers : Avoid concomitant use of moderate CYP3A inducers. If a moderate CYP inducer cannot be avoided, increase ripretinib dose frequency to twice daily. ( 2.3 , 7.1 )
7.1Effect of Other Drugs on QINLOCK Table 4 includes drug interactions that affect the pharmacokinetics of ripretinib. Table 4: Drug Interactions that Affect QINLOCK Strong CYP3A Inhibitors Clinical Impact Coadministration of QINLOCK with a strong CYP3A inhibitor increased the exposure of ripretinib and its active metabolite (DP-5439), which may increase the risk of adverse reactions [see Clinical Pharmacology ( 12.3 )]. Prevention or Management Monitor patients more frequently for adverse reactions.
Strong and Moderate CYP3A Inducers Clinical Impact Coadministration of QINLOCK with a strong CYP3A inducer decreased the exposure of ripretinib and its active metabolite (DP-5439), which may decrease QINLOCK anti-tumor activity [see Clinical Pharmacology ( 12.3 )] . Coadministration of QINLOCK with moderate CYP3A inducers is predicted to decrease the exposure of ripretinib and its active metabolite (DP-5439), which may decrease QINLOCK anti-tumor activity [see Clinical Pharmacology ( 12.3 )] . Prevention or Management Avoid concomitant use of QINLOCK with strong CYP3A inducers.
Avoid concomitant use of QINLOCK with moderate CYP3A inducers. If a moderate CYP3A inducer cannot be avoided, increase QINLOCK dosing frequency from the recommended dose of 150 mg once daily to 150 mg twice daily during the co-administration period. Monitor for clinical response and tolerability [see Dosage and Administration ( 2.3 )] .
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Lactation : Advise not to breastfeed. ( 8.2 )
8.1Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , QINLOCK can cause fetal harm when administered to a pregnant woman. There are no available data on the use of QINLOCK in pregnant women to inform a drug-associated risk. Administration of ripretinib to pregnant rats and rabbits during the period of organogenesis resulted in malformations primarily associated with the cardiovascular and skeletal systems, anatomic variations, reduced fetal body weight, and increased post-implantation loss at maternal exposures that were approximately equal to the human exposure at the recommended dose of 150 mg (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 Animal Data In an embryo-fetal development study investigating daily doses of ripretinib administered during the period of organogenesis in rats, ripretinib resulted in malformations primarily associated with the cardiovascular and skeletal systems, including interrupted or retroesophageal aortic arch and retroesophageal subclavian artery, fusion of the exoccipital bone to the first cervical vertebra, branched and fused ribs, anomalies of the cervical, thoracic, caudal, and sacral vertebrae, absent forepaw phalanges, and absent metacarpals at a dose of 20 mg/kg/day (approximately one half of the human exposure at the recommended dose of 150 mg).
An increased incidence of anatomic variations were also observed at 20 mg/kg/day. Variations included malpositioned carotid and subclavian artery origins, malpositioned subclavian artery, absent or elongated innominate artery, misshapen and nodulated ribs, bipartite, incompletely ossified, or unossified vertebral centra, small or misshapen vertebral arches, and reductions in ossified forelimb and hindlimb phalanges, hindlimb metatarsals, and caudal vertebrae. In a preliminary embryo-fetal development study investigating the administration of ripretinib in rabbits during the period of organogenesis, ripretinib resulted in total loss of pregnancy at doses of 150 mg/kg (approximately 3.5 times the human exposure at the recommended dose of 150 mg).
At a dose of 40 mg/kg (approximately 2.1 times the human exposure at the recommended dose of 150 mg), toxicities included increased post-implantation loss and decreased fetal body weights.
8.2Lactation Risk Summary There are no data regarding the presence of ripretinib or its metabolites in either human milk or its effects on a breastfed child or on milk production. Because of the potential for serious adverse reactions in the breastfed child, advise women not to breastfeed during treatment with QINLOCK and for 1 week after the last dose.
8.3Females and Males of Reproductive Potential QINLOCK can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations ( 8.1 )] . Pregnancy Testing Verify pregnancy status of females of reproductive potential prior to the initiation of QINLOCK [see Use in Specific Populations ( 8.1 )] . Contraception Females Advise females of reproductive potential to use effective contraception during treatment and for 1 week after the last dose.
Males Advise males with female partners of reproductive potential to use effective contraception during treatment and for 1 week after the last dose. Infertility Based on findings from animal studies, QINLOCK may impair fertility in males of reproductive potential [see Nonclinical Toxicology ( 13.1 )] .
8.4Pediatric Use The safety and effectiveness of QINLOCK in pediatric patients have not been established. Animal Toxicity Data In 13-week repeat-dose studies in rats there were dose-dependent findings of increased osteoblastic surface and decreased trabeculae of the…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , QINLOCK can cause fetal harm when administered to a pregnant woman. There are no available data on the use of QINLOCK in pregnant women to inform a drug-associated risk. Administration of ripretinib to pregnant rats and rabbits during the period of organogenesis resulted in malformations primarily associated with the cardiovascular and skeletal systems, anatomic variations, reduced fetal body weight, and increased post-implantation loss at maternal exposures that were approximately equal to the human exposure at the recommended dose of 150 mg (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 Animal Data In an embryo-fetal development study investigating daily doses of ripretinib administered during the period of organogenesis in rats, ripretinib resulted in malformations primarily associated with the cardiovascular and skeletal systems, including interrupted or retroesophageal aortic arch and retroesophageal subclavian artery, fusion of the exoccipital bone to the first cervical vertebra, branched and fused ribs, anomalies of the cervical, thoracic, caudal, and sacral vertebrae, absent forepaw phalanges, and absent metacarpals at a dose of 20 mg/kg/day (approximately one half of the human exposure at the recommended dose of 150 mg).
An increased incidence of anatomic variations were also observed at 20 mg/kg/day. Variations included malpositioned carotid and subclavian artery origins, malpositioned subclavian artery, absent or elongated innominate artery, misshapen and nodulated ribs, bipartite, incompletely ossified, or unossified vertebral centra, small or misshapen vertebral arches, and reductions in ossified forelimb and hindlimb phalanges, hindlimb metatarsals, and caudal vertebrae. In a preliminary embryo-fetal development study investigating the administration of ripretinib in rabbits during the period of organogenesis, ripretinib resulted in total loss of pregnancy at doses of 150 mg/kg (approximately 3.5 times the human exposure at the recommended dose of 150 mg).
At a dose of 40 mg/kg (approximately 2.1 times the human exposure at the recommended dose of 150 mg), toxicities included increased post-implantation loss and decreased fetal body weights.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of QINLOCK in pediatric patients have not been established. Animal Toxicity Data In 13-week repeat-dose studies in rats there were dose-dependent findings of increased osteoblastic surface and decreased trabeculae of the femur at doses ≥30 mg/kg/day (approximately one half of the human exposure at the recommended dose of 150 mg). There were additional findings of missing or discolored teeth that were accompanied by dose-dependent incisor degeneration at doses ≥30 mg/kg/day.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the 85 patients in INVICTUS who received QINLOCK 150 mg orally once daily, 24% were between 65 to 74 years of age and 9% were 75 years of age or older. Clinical studies of QINLOCK did not include sufficient numbers of patients aged 65 and older to determine whether they respond differently from younger patients.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Ripretinib is a tyrosine kinase inhibitor that inhibits KIT proto-oncogene receptor tyrosine kinase (KIT) and platelet derived growth factor receptor A (PDGFRA) kinase, including wild type, primary, and secondary mutations. Ripretinib also inhibits other kinases in vitro, such as PDGFRB, TIE2, VEGFR2, and BRAF.
12.2Pharmacodynamics Exposure-Response Relationships Ripretinib exposure-response relationships and the time course of pharmacodynamics have not been fully characterized. Cardiac Electrophysiology No large mean increase in QTc interval (i.e. >20 ms) was detected following treatment with QINLOCK at the recommended dose of 150 mg taken orally once daily.
12.3Pharmacokinetics The pharmacokinetics of ripretinib and its equally active metabolite (DP-5439) were characterized in clinical studies. In patients with advanced malignancies, ripretinib AUC 0-24h increased proportionally over a dose range of 20-250 mg (0.13 to 1.67 times the recommended dose), but C max was less than dose proportional; DP-5439 C max and AUC 0-24h were less than dose proportional within the dose range of 50-250 mg (0.33 to 1.67 times the recommended dose). No clinically significant differences in the C max and AUC 0-24h were observed between administration of QINLOCK with a high-fat meal (150, 250, and 500-600 calories from protein, carbohydrate, and fat, respectively) and under fasted conditions.
The pharmacokinetic parameters of ripretinib and DP-5439 are summarized in Table 5 . Table 5: Pharmacokinetic Parameters of Ripretinib and DP-5439 a. Estimated based on cycle 1, day 15 b.
After a single oral dose of 150 mg CV=coefficient of variation; C max =maximum plasma concentration; AUC 0-12h =area under the plasma concentration-time curve from time zero to 12 hours; AUC 0-24h =area under the plasma concentration-time curve from time zero to 24 hours; T max =time to maximum concentration Parameter Ripretinib DP-5439 General Information Steady state exposure following QINLOCK 150 mg once daily [Mean (CV%)] C max (ng/mL) 761 (32) 804 (46) AUC 0-12h (ng•h/mL) 5678 (32) 7138 (44) Time to steady state [Days] 14 14 Accumulation ratio (AUC 0-12h ) [Mean (CV%)] a 1.7 (55) 5.29 (49) Absorption T max [Median in hours] b 4
15.6Distribution Plasma protein binding (in vitro) Human serum albumin 99.8% 99.7% α-1 acid glycoprotein 99.4% >99.8% Steady state apparent volume of distribution, L [Mean (CV%)] b 307 (39) 507 (51) Elimination Apparent clearance, L/hr [Mean (CV%)] b 15.3 (45) 17.5 (63) Half-life, hours [Mean (CV%)] b 14.8 (30) 17.8 (23) Metabolism Metabolic pathways Major CYP3A4 CYP3A4 Minor CYP2C8 and CYP2D6 CYP2C8, CYP2E1 and CYP2D6 Excretion Excretion pathways Feces 34% 6% Urine 0.02% 0.1% Specific Populations No clinically significant differences in the pharmacokinetics of ripretinib were observed based on age (19 to 87 years), sex, race (White, Black, and Asian), body weight (39 to 138 kg), tumor (GIST or other solid tumors), prior gastrectomy, mild to moderate renal impairment (CLcr 30 to <90 mL/min estimated by Cockcroft-Gault), and mild hepatic impairment (total bilirubin ≤ULN and AST >ULN or total bilirubin 1 to 1.5 × ULN and AST any).
The effects of severe renal impairment (CLcr 15 to 29 mL/min) on the pharmacokinetics of ripretinib have not been studied. Patients with Hepatic Impairment In subjects with mild hepatic impairment, there were no clinically significant changes in AUC 0-last and C max when compared to matched healthy subjects. In subjects with moderate hepatic impairment, ripretinib AUC 0-last increased 2-fold while C max was unchanged when compared to matched healthy subjects.
The combined AUC 0-last of ripretinib and DP-5439 increased 1.5-fold. In subjects with severe hepatic impairment, ripretinib AUC 0-last increased 2.6-fold and C max decreased by 24% when compared to matched healthy subjects. The combined AUC 0-last of ripretinib and DP-5439 increased by 1.4-fold.
The observed magn…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Ripretinib is a tyrosine kinase inhibitor that inhibits KIT proto-oncogene receptor tyrosine kinase (KIT) and platelet derived growth factor receptor A (PDGFRA) kinase, including wild type, primary, and secondary mutations. Ripretinib also inhibits other kinases in vitro, such as PDGFRB, TIE2, VEGFR2, and BRAF.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING QINLOCK 50 mg tablets are white to off-white, oval shaped, and debossed with “DC1” on one side. 90-count bottles NDC 73207-101-30 Dispense in original container only. Store in the original container with the desiccant to protect from moisture and light.
Replace cap securely each time after opening. Do not discard desiccant. Store at 20°C to 25°C (68°F to 77°F); excursion permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature] .
📋 Description ▾
11 DESCRIPTION Ripretinib is a kinase inhibitor. The chemical name of ripretinib is 1-(4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl]-2-fluorophenyl)-3-phenylurea. The molecular formula is C 24 H 21 BrFN 5 O 2 and the molecular weight is 510.36 g/mol.
The chemical structure of ripretinib is shown below: Ripretinib is a white to off-white crystalline solid. Ripretinib is a lipophilic, weak base, and practically insoluble in aqueous media. QINLOCK is available as a white to off-white, oval tablets for oral use containing 50 mg of ripretinib.
The tablet is debossed with “DC1” on one side. Each tablet contains the following inactive ingredients: crospovidone, hypromellose acetate succinate, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and silicon dioxide. Figure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling ( Patient Information ). Palmar-Plantar Erythrodysesthesia Syndrome Advise patients to contact their healthcare provider immediately if they experience severe skin changes [see Warnings and Precautions ( 5.1 )] . New Primary Cutaneous Malignancies Advise patients to contact their healthcare provider immediately for change in or development of new skin lesions [see Warnings and Precautions ( 5.2 )] .
Hypertension Advise patients that hypertension may develop during treatment with QINLOCK and that blood pressure should be monitored regularly during treatment [ see Warnings and Precautions ( 5.3 )] . Cardiac Dysfunction Advise patients that cardiac failure may develop during treatment with QINLOCK and that signs or symptoms of cardiac failure should be regularly monitored during treatment. Advise patients to contact their healthcare provider immediately for signs or symptoms of cardiac dysfunction [see Warnings and Precautions ( 5.4 )] .
Risk of Impaired Wound Healing Advise patients that QINLOCK may impair wound healing. Advise patients to inform their healthcare provider of any planned surgical procedure [see Warnings and Precautions ( 5.5 )] . Photosensitivity Inform patients that there is a potential risk of photosensitivity reactions with QINLOCK.
Advise patients to limit direct ultraviolet exposure by using sunscreen and protective clothing during treatment with QINLOCK [see Warnings and Precautions ( 5.6 )]. Embryo-Fetal Toxicity Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to inform their healthcare provider of a known or suspected pregnancy [see Warnings and Precautions ( 5.7 ), Use in Specific Populations ( 8.1 )] .
Advise females of reproductive potential to use effective contraception during treatment with QINLOCK and for 1 week after the last dose [see Use in Specific Populations ( 8.3 )]. Advise males with female partners of reproductive potential to use effective contraception during treatment with QINLOCK and for 1 week after the last dose [see Use in Specific Populations ( 8.3 ), Nonclinical Toxicology ( 13.1 )] . Lactation Advise females not to breastfeed during treatment with QINLOCK and for 1 week after the last dose [see Use in Specific Populations ( 8.2 )] .
Infertility Advise males of reproductive potential that QINLOCK may impair fertility [see Use in Specific Populations ( 8.3 ), Nonclinical Toxicology ( 13.1 ) ] . Drug Interactions Advise patients to inform their healthcare provider of all concomitant medications, including prescription medicines, over-the-counter drugs, vitamins, and herbal products [see Drug Interactions ( 7.1 )] . Dosage and Administration Instruct patients to take QINLOCK at the same time each day (once daily) with or without food.
Advise patients to swallow tablets whole. Inform patients about what to do in the event they miss a dose or vomit after taking a dose of QINLOCK [see Dosage and Administration ( 2.1 ) ] . Storage Instructions Store QINLOCK in the original container at room temperature between 20ºC to 25ºC (68ºF to 77ºF).
Manufactured for and marketed by: Deciphera Pharmaceuticals, LLC 200 Smith Street, Waltham, MA 02451