ripretinib

Contraindicated in:

OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Uncontrolled hypertension (do not initiate therapy until BP adequately controlled);
Left ventricular ejection fraction (LVEF) <50%;
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CNS: headache

CV: hypertension, peripheral edema, HF, MI

Derm: alopecia, dry skin, palmar-plantar erythrodysesthesia syndrome , pruritus, CUTANEOUS SQUAMOUS CELL CARCINOMA , impaired wound healing, MELANOMA, photosensitivity reactions

F and E: hypocalcemia, hyponatremia, hypophosphatemia

GI: ↑amylase, ↑lipase, ↑liver enzymes, abdominal pain, constipation, diarrhea, hyperbilirubinemia, nausea, stomatitis, vomiting

GU: ↓fertility (men), ↑serum creatinine

Hemat: ↑activated partial thromboplastin time, ↑INR, neutropenia

Metab: ↓appetite, weight loss, hypertriglyceridemia

MS: ↓creatine kinase, arthralgia, muscle spasms, myalgia

Neuro: fatigue

Resp: dyspnea

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A4 inhibitors, including itraconazole, may ↑ levels of ripretinib and DP-5439 and risk of toxicity.
Strong CYP3A4 inducers, including rifampin, may ↓ levels of ripretinib and DP-5439 and effectiveness; avoid concurrent use.
Moderate CYP3A4 inducers, including efavirenz, may ↓ levels of ripretinib and DP-5439 and effectiveness; avoid concurrent use. If concurrent use unavoidable, ↑ ripretinib dose.

Drug-Natural Products:

St. John's wort may ↓ levels of ripretinib and DP-5439 and effectiveness; avoid concurrent use.

Drug-Food:

Grapefruit juice may ↑ levels of ripretinib and DP-5439 and risk of toxicity.

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

PO (Adults ): 150 mg once daily until disease progression or unacceptable toxicity. Concurrent use of moderate CYP3A4 inducer: 150 mg twice daily until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Tyrosine kinase inhibitor that inhibits KIT proto-oncogene receptor tyrosine kinase and platelet derived growth factor receptor A kinase, including wild type, primary, and secondary mutations.

Therapeutic effects:

Improved progression-free survival.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors, platelet-derived growth factor receptor alpha blockers

Pharmacokinetics ⬆ ⬇

Absorption: Unknown.

Distribution: Extensively distributed to extravascular tissues.

Protein Binding: 99.8%.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A4 isoenzyme (and to a minor extent via the CYP2C8 and CYP2D6 isoenzymes) to an active metabolite (DP-5439). DP-5439 is primarily metabolized in the liver via the CYP3A4 isoenzyme (and to a minor extent via the CYP2C8, CYP2E1, and CYP2D6 isoenzymes). Ripretinib and DP-5439 primarily excreted in feces (34% and 6%, respectively).

Half-Life: Ripretinib: 14.8 hr; DP-5439: 17.8 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	Ripretinib: 4 hr; DP-5439: 15.6 hr	Unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Advise patients to take a missed dose if <8 hr since missed dose. Do not take additional dose if vomiting occurs after taking ripretinib; omit and continue with next scheduled dose.
Inform patient to stop ripretinib ≥1 wk prior to and for ≥2 wk following surgery until adequate wound healing occurs.
Advise patients to limit direct UV exposure during therapy and for ≥1 wk after discontinuation.
Advise patient to notify health care professional immediately if they experience skin changes or new lesions, including but not limited to palms and bottom of feet.
Advise patient to notify health care professional immediately if severe hypertension or cardiac dysfunction (difficulty breathing with exercise or sleep, swelling of lower extremities, fatigue) occur.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: May cause fetal harm. Both women and men with partners of reproductive potential should use effective contraception during therapy and for 1 wk after last dose. Advise women to avoid breastfeeding during therapy and for 1 wk after last dose. May impair fertility in men of reproductive potential.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

59116- Cambrex Charles City, Inc
- 59116-5330-
  - 59116-5330-3- 50 kg in 1 DRUM (59116-5330-3)

59116- Cambrex Charles City, Inc
- 59116-5331-
  - 59116-5331-3- 50 kg in 1 DRUM (59116-5331-3)

59116- Cambrex Charles City, Inc
- 59116-5332-
  - 59116-5332-3- 50 kg in 1 DRUM (59116-5332-3)

59116- Cambrex Charles City, Inc
- 59116-5333-
  59116-5333-3- 50 kg in 1 DRUM (59116-5333-3)

73207- Deciphera Pharmaceuticals, LLC
- 73207-101- QINLOCK
  73207-101-30- 1 BOTTLE in 1 CARTON (73207-101-30) / 90 TABLET in 1 BOTTLE

73207- Deciphera Pharmaceuticals, LLC
- 73207-101- QINLOCK
  - 73207-101-31- 1 BOTTLE in 1 CARTON (73207-101-31) / 30 TABLET in 1 BOTTLE

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇