Ripretinib

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.

• 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.

• None. None.contraindicated

Recommended Dosage : 150 mg orally once daily with or without food. ( 2.1 ) 2.1 Recommended 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. 2.2 Dosage 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.

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 ) 5.1 Palmar-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 )].

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. 6.1 Clinical 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.

Lactation : Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy 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.

Metabolism

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).

• May 15, 2020NDANDA213973Deciphera Pharms

1. 1Fatigue66413%
2. 2Alopecia57511%
3. 3Death3737.5%
4. 4Underdose3667.3%
5. 5Extra Dose Administered3577.1%
6. 6Nausea3286.6%
7. 7Drug Ineffective3246.5%
8. 8Hospitalisation3136.3%
9. 9Disease Progression2905.8%
10. 10Constipation2865.7%
11. 11Pain2765.5%
12. 12Diarrhoea2725.4%
13. 13Neoplasm Progression2665.3%
14. 14Inappropriate Schedule Of Product Administration2585.2%
15. 15Product Use In Unapproved Indication2585.2%

The 10 most recently updated of 19 ClinicalTrials.gov registrations naming Ripretinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of Inlexisertib (DCC-3116) in Combination With Anticancer Therapies in Participants With Advanced Malignancies
  Recruiting · Phase 1 · Phase 2 · Interventional · 94 enrolled · Deciphera Pharmaceuticals, LLC
  NCT05957367updated 2026-06-02
• First-in-human Study of IDRX-42 in Participants With Metastatic and/or Unresectable Gastrointestinal Stromal Tumors
  Recruiting · Phase 1 · Interventional · 278 enrolled · IDRX, Inc., a wholly owned subsidiary of GSK, LLC
  NCT05489237updated 2026-05-04
• A Study to Assess DCC-2618 and Sunitinib in Patients With Advanced GIST After Treatment With Imatinib
  Completed · Phase 2 · Interventional · 108 enrolled · Zai Lab (Shanghai) Co., Ltd.
  NCT04633122updated 2026-04-03
• A Study of Ripretinib vs Sunitinib in Advanced GIST Patients After Treatment With Imatinib
  Active not recruiting · Phase 3 · Interventional · 453 enrolled · Deciphera Pharmaceuticals, LLC
  NCT03673501updated 2026-02-05
• A Study of Ripretinib vs Sunitinib in Patients With Advanced GIST With Specific KIT Exon Mutations Who Were Previously Treated With Imatinib
  Active not recruiting · Phase 3 · Interventional · 54 enrolled · Deciphera Pharmaceuticals, LLC
  NCT05734105updated 2025-12-17
• Ripretinib (QINLOCK®) According to Current SmPC
  Completed · Observational · 10 enrolled · iOMEDICO AG
  NCT06619275updated 2025-12-05
• Resistance Profiling Using Functional Imaging and Next Generation Sequencing in Refractory Gastrointestinal Stomal Tumors (GIST)
  Not yet recruiting · Observational · 40 enrolled · Universität Duisburg-Essen
  NCT07109024updated 2025-08-19
• A Study of DCC-2618 (Ripretinib) In Patients With With Advanced Gastrointestinal Stromal Tumors (GIST)
  Completed · Phase 2 · Interventional · 39 enrolled · Zai Lab (Shanghai) Co., Ltd.
  NCT04282980updated 2025-03-03
• The Correlation Between Ripretinib Exposure and the Efficacy and Safety in Patients with Advanced GISTs
  Unknown · Observational · 60 enrolled · First Affiliated Hospital, Sun Yat-Sen University
  NCT06431451updated 2025-02-26
• A Drug-Drug Interaction Study to Evaluate the Effect of Ripretinib on the Pharmacokinetics of a CYP2C8 Probe Substrate in Patients with Advanced GIST
  Completed · Phase 1 · Interventional · 13 enrolled · Deciphera Pharmaceuticals, LLC
  NCT04530981updated 2024-09-19

Frequently asked questions

How does Ripretinib work?

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.

What is Ripretinib used for?

According to FDA labeling, Ripretinib carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Ripretinib?

Ripretinib is classified as Other protein kinase inhibitors, Kinase Inhibitor, Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 2C8 Inhibitors, P-Glycoprotein Inhibitors, Platelet-derived Growth Factor alpha Receptor Inhibitors, Stem Cell Factor (KIT) Receptor Inhibitors, Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Ripretinib?

Ripretinib is marketed under brand names including Qinlock.

What are the contraindications for Ripretinib?

Ripretinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.