Qinlock

— THERAPEUTIC CATEGORIES —
  • Colorectal and other GI cancers

Qinlock Generic Name & Formulations

General Description

Ripretinib 50mg; tabs.

Pharmacological Class

Tyrosine kinase inhibitor.

How Supplied

Tabs—90

Generic Availability

NO

Mechanism of Action

Ripretinib 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 Indications

Indications

In adults with advanced gastrointestinal stromal tumor (GIST) who have received prior treatment with ≥3 kinase inhibitors, including imatinib.

Qinlock Dosage and Administration

Adult

Swallow whole. 150mg once daily until disease progression or unacceptable toxicity. Concomitant moderate CYP3A4 inducer (if unavoidable): give 150mg twice daily. Dose modifications: see full labeling.

Children

Not established.

Qinlock Contraindications

Not Applicable

Qinlock Boxed Warnings

Not Applicable

Qinlock Warnings/Precautions

Warnings/Precautions

Risk of new primary cutaneous malignancies. Perform skin exams prior to initiation and during therapy. Manage suspicious skin lesions with excision and dermatopathologic evaluation. Uncontrolled hypertension: do not initiate. Control BP prior to initiation; monitor and treat during therapy as appropriate. Cardiac dysfunction. Assess ejection fraction by echocardiogram or MUGA scan prior to initiation, during therapy, and as clinically indicated. Permanently discontinue if Grade 3/4 left ventricular systolic dysfunction occurs. Impaired wound healing: withhold for ≥1 week prior to elective surgery; do not give for ≥2 weeks after major surgery and until adequate healing. Safety of resuming therapy after resolution of wound healing complications has not been established. Photosensitivity: limit UV exposure during and for at least 1 week after discontinuation. Moderate or severe hepatic impairment. Severe renal impairment. Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective contraception during and for ≥1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for ≥1 week after the last dose).

Qinlock Pharmacokinetics

Absorption

Median Tmax: 4 hours (after a single 150 mg oral dose).

Distribution

Plasma protein bound: 99.8% (serum albumin); 99.4% (alpha-1 acid glycoprotein). Apparent volume of distribution at steady state: 307 L.

Metabolism

CYP3A4 (major), CYP2C8, CYP2D6.

Elimination

Fecal (34%), renal (0.02%). Half-life: ~14.8 hours. Apparent clearance: 15.3 L/hr.

Qinlock Interactions

Interactions

Potentiated by strong CYP3A4 inhibitors; monitor frequently. Antagonized by strong CYP3A4 inducers; avoid concomitant use. May be antagonized by moderate CYP3A4 inducers; avoid concomitant use; if unavoidable, increase dosing frequency (see Adult dose).

Qinlock Adverse Reactions

Adverse Reactions

Alopecia, fatigue, nausea, abdominal pain, constipation, myalgia, diarrhea, decreased appetite, palmar-plantar erythrodysesthesia, vomiting; lab abnormalities (eg, increased lipase, decreased phosphate).

Qinlock Clinical Trials

See Literature

Qinlock Note

Not Applicable

Qinlock Patient Counseling

See Literature

Images