Vimseltinib

Vimseltinib is a prescription medication indicated for the treatment of adult patients with symptomatic tenosynovial giant cell tumor (TGCT) for which surgical resection will potentially cause worsening functional limitation or severe morbidity. 

• Vimseltinib is available under the following different brand names: Romvimza.

Common side effects of Vimseltinib include:

• fatigue
• rash
• pruritus
• periorbital edema
• face edema
• peripheral edema
• increased aspartate aminotransferase levels
• increased alanine aminotransferase levels
• increased cholesterol levels 
• decreased neutrophil count
• decreased leukocyte count

Serious side effects of Vimseltinib include:

• hepatotoxicity
• allergic reactions to FD&C Yellow No. 5 and FD&C Yellow No. 6

Rare side effects of Vimseltinib include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats, fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Capsule

• 14 mg
• 20 mg
• 30 mg

TGCT

Adult dosage

• 30 mg orally 2 two times every week
• Separate doses for at least 72 hours

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

Drug interaction overview

• Vimseltinib is a P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and organic cation transporter 2 (OCT2) inhibitor
• P-gp substrates
  • Follow P-gp substrate recommendations for use with P-gp inhibitors
  • Alternatively, avoid coadministration or administer vimseltinib at least 4 hr before P-gp substrate
• BCRP substrates
  • Follow BCRP substrate recommendations for use with BCRP inhibitors
  • Alternatively, avoid coadministration
• OCT2 substrates
  • Follow OCT2 substrate recommendations for use with OCT2 inhibitors
  • Alternatively, avoid coadministration

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Vimseltinib?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Vimseltinib?”

Cautions

• Hepatotoxicity
  • Serious and fatal liver injury not reported; however, cases of serious and fatal liver injury occurred with the use of another CSF1R inhibitor
  • Avoid use in patients with pre-existing increased serum transaminases, TB or direct bilirubin increased more than ULN, or active liver or biliary tract disease (e.g., increased ALP)
  • Monitor LFTs (e.g., AST, ALT, TB, direct bilirubin, ALP, and GGT) before starting therapy, twice monthly for the first 2 months, once every 3 months for the first year of therapy, and as clinically indicated thereafter
  • Hold, reduce dose, or permanently discontinue based on hepatotoxicity severity
• Allergic reactions to FD&C Yellow No.5 and No.6
  • FD&C Yellow No. 5 (tartrazine) in 20-mg capsules may cause allergic reactions (e.g., bronchial asthma) in certain susceptible patients
  • The overall incidence of tartrazine sensitivity in the general population is low; patients with aspirin sensitivity may be at increased risk
  • FD&C Yellow No.6 (Sunset Yellow FCF) in 14-mg and 20-mg capsules may also cause allergic reactions
• Increased serum creatinine (SCr) without affecting renal function
  • SCr increased by a mean of 19 micromol/L and reached a maximum mean increase by 10.4 weeks compared to baseline in a clinical trial
  • Increased SCr may not be associated with changes in renal function; SCr increases were reversible upon drug discontinuation
  • Increased SCr may be due to the inhibition of renal tubular secretion transporters (e.g., OCT2 and MATE1)
  • Use alternate measures not based on serum creatinine to assess renal function during therapy
• Embryo-fetal toxicity
  • May cause fetal harm when administered during pregnancy
  • Advise pregnant patients on potential fetal risks
  • Effective contraception use is recommended during and after therapy in females of reproductive potential and males with female partners of reproductive potential

Pregnancy and Lactation

• May cause fetal harm when administered during pregnancy, based on mechanism of action and animal data
• No available data on use in pregnant patients to evaluate drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
• Advise pregnant women of potential fetal risks
• Verify pregnancy status in females of reproductive potential before starting therapy

Contraception requirements

• Effective contraception is recommended during therapy and for 1 month after the last dose in females of reproductive potential and males with female partners of reproductive potential

Infertility

• May impair fertility in males and females, based on findings from animal studies

Lactation

• No data regarding the presence of human or animal milk, its effects on breastfed children, or milk production
• Due to the potential for serious adverse reactions in breastfed children, patients should not breastfeed during therapy and for 1 month after the last dose