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Brand Name :
N/A
Synonyms :
fulzerasib
Class :
Antineoplastic, KRAS inhibitor
Brand Name :
N/A
Synonyms :
fulzerasib
Class :
Antineoplastic, KRAS inhibitor
Dosage forms & strengthsÂ
Injectable solution Â
1 mg/kg Â
3 mg/kg Â
10 mg/kg Â
Oral Â
0.3 mpk Â
KRAS G12C-mutant driven non-small cell lung cancer (NSCLC) (off-label)
With parenteral minimal effective dosages of 1 mg per kg, 3 mg per kg, 10 mg per kg, and 2 mg per kg, respectively, this medication showed strong anti-tumor action in human lung adenocarcinoma, multiple KRAS G12C-mutant tumor models, colonic adenocarcinoma, and lung cancer models in a phase I trial.
:
Dose Adjustments
Limited data is available
Safety and efficacy are not seen in pediatrics Â
Refer to the adult dosingÂ
Actions and Spectrum: Â
Actions: Â
Fulzerasib inhibits the growth of KRAS G12C-mutant tumor cells by blocking the KRAS pathway through covalently inhibiting nucleotide exchange on KRAS G12C, trapping it in a GDP-bound form.Â
Spectrum: Â
Strong anti-cancer benefits were demonstrated by this drug in several tumour models, including colonic adenocarcinoma and lung cancer, especially in those with the KRAS G12C mutation.Â
Limited data is availableÂ
Limited data is available Â
Contraindication/Caution: Â
Contraindications Â
Hypersensitivity Â
Cautions Â
Renal impairment Â
Hepatic impairment Â
Drug interactions Â
Pregnancy  Â
Breastfeeding Â
Pregnancy/Lactation:Â
Pregnancy consideration:  Â
No data is available regarding the administration of the drug during pregnancy. Â
Breastfeeding warnings:  Â
No data is available regarding the excretion of drug in breast milk. Â
Pregnancy category: Â
Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. Â
<b>Category B: There was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. Â
Category C: There was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    Â
Category D: Adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    Â
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    Â
Category N: No data is available for the drug under this category. Â
Pharmacology: Â
Fulzerasib blocks KRAS G12C-mutant tumor cell growth by inhibiting it signaling pathway. It does this by trapping KRAS in a GDP-bound form and preventing nucleotide exchange.Â
Pharmacodynamics: Â
Fulzerasib traps KRAS G12C in inactive state by blocking nucleotide exchange, limiting tumor cell growth.Â
Pharmacokinetics: Â
Limited data is available Â
Administration: Â
Administered parenterally, presently, it is in phase 1 study. Â
Patient information leaflet Â
Generic Name: fulzerasib Â
Pronounced: Full-zuh-rah-sib Â
Why do we use fulzerasib? Â
Fulzerasib, a cancer drug, is being studied to treat non-small cell lung cancer by stopping the growth of KRAS G12C-mutant tumor cells. It blocks the KRAS pathway signaling by trapping KRAS in its GDP-bound form through covalent blockade of nucleotide exchange.Â
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