Ripretinib

QINLOCK

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Pronunciation: rip-RE-tin-ib (KIN-lok)

Ripretinib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Ripretinib ballicule

What it isAn oral switch-control tyrosine kinase inhibitor that broadly inhibits KIT and PDGFRA, including many secondary resistance mutations.

Why this oneIt is approved for fourth-line advanced gastrointestinal stromal tumor after progression on three or more prior kinase inhibitors including imatinib.

What limits itPalmar-plantar erythrodysesthesia, hypertension, cardiac dysfunction, and new primary cutaneous malignancies require monitoring.

Ripretinib molecular structure (skeletal formula) — Molecular structure: Ripretinib

FDA label

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FDA dosing	Population	Start	Target	Max
Advanced gastrointestinal stromal tumor (GIST), previously treated (imatinib/sunitinib/regorafenib)	Adults	150 mg QD	150 mg QD until progression or unacceptable toxicity	150 mg QD (150 mg BID only during unavoidable moderate CYP3A inducer co-use)

Renal Undefined

Hepatic No dose adjustment (Child-Pugh A, B, or C)

Instructions

Swallow tablets whole, with or without food, same time each day
Missed dose: take if <8 h since scheduled time; if vomiting occurs, do not redose — take next scheduled dose
Dose reduction for adverse reactions: 100 mg QD; discontinue if 100 mg QD not tolerated
Withhold/modify for PPES, grade 3 hypertension, grade 2-3 arthralgia/myalgia, other grade 3-4 reactions per Table 1; permanently discontinue for grade 4 hypertension or grade 3-4 LV systolic dysfunction
Avoid moderate CYP3A inducers; if unavoidable, increase to 150 mg BID, then resume 150 mg QD 14 days after inducer stops
Withhold ≥1 wk before elective surgery; do not give for ≥2 wks after major surgery and until adequate wound healing

Available strengths

tab 50 mg

Cautions

Palmar-plantar erythrodysesthesia syndrome (21%) — withhold/dose-reduce by severity
New primary cutaneous malignancies (cuSCC, melanoma) — dermatologic evaluation at baseline and routinely
Hypertension (14%, grade 3 7%) — do not initiate with uncontrolled hypertension; monitor BP
Cardiac dysfunction — assess ejection fraction before and during treatment; permanently discontinue for grade 3-4 LV systolic dysfunction
Impaired wound healing — hold around surgery
Photosensitivity — limit direct UV exposure during and ≥1 wk after treatment
Embryo-fetal toxicity — effective contraception (both sexes) during and 1 wk after treatment; may impair male fertility

Adverse reactions

Alopecia
Fatigue
Nausea
Abdominal pain
Constipation
Myalgia
Diarrhea
Decreased appetite
Palmar-plantar erythrodysesthesia
Vomiting
Lab: increased lipase, decreased phosphate (grade 3-4 ≥4%)

Pregnancy Can cause fetal harm (animal malformations at ~half human exposure); verify pregnancy status before start; no human data

Lactation Do not breastfeed during treatment and for 1 week after last dose

Cost

Ripretinib (QINLOCK)

Strength		#/mo	generic $/mo	CostPlus
50 mg	tab	30 qd		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Ripretinib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2042 est.

NO BOXED WARNINGS

Principal riskNo FDA boxed warning.

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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