Elunate® (HUTCHMED) Tazverik® (HUTCHMED)
New Product
HKPharm J Volume 31 (2), May-Aug-2024 (2024-09-23): P.57
Elunate®
(HUTCHMED)
Active Ingredients
Fruquintinib
Pharmacological Properties
Fruquintinib is a selective inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2 and 3, and has an inhibitory effect on VEGFR kinase activity, VEGFR 2/3 phosphorylation in cells and tissues, endothelial cell proliferation, and lumen formation, micro-angiogenesis in chick embryo chorioallantoic membrane model, and tumor angiogenesis, thereby inhibiting tumor growth.
Indication
As monotherapy is indicated for patients with metastatic colorectal cancer (mCRC) who have previously received fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy, and those who have previously received or are not suitable for receiving anti-vascular endothelial growth factor (VEGF) therapy or anti-epidermal growth factor receptor (EGFR) therapy (RAS wild-type).
Dosage Forms and Strengths
1mg and 5 mg capsules
Dosage Administration
The recommended dose is 5mg once daily, for three consecutive weeks followed by one week of drug free period (Every 4 weeks as one treatment cycle).
This product may be taken with food or on empty stomach, and it must be swallowed whole. It is recommended to take the drug at the same time each day. If the patient vomits after administering the drug, there is no need to make up for the dose; if a dose is missed, instruct the patient not to make up for the dose in the next day, but to take the next dose at its next scheduled time.
Contraindications
Hypersensitivity to the active substance or to any of the excipients of fruquintinib capsule.
Patients with severe active haemorrhage, active gastrointestinal ulcer, unhealed gastrointestinal perforation or gastrointestinal fistula are prohibited from using this product. Patients with severe hepatic impairment and renal impairment are prohibited from using this product. Pregnant, breastfeeding women are prohibited from using this product.
Adverse Reactions
The common (incidence ≥ 2%) Grade ≥3 adverse drug reactions were hypertension, hand-foot skin reaction, proteinuria, platelet count decreased, hepatic function abnormal, blood bilirubin increased, abdominal pain/abdominal discomfort, diarrhoea, fatigue/asthenia, decreased appetite and haemorrhage.
Drug Interactions
No dose adjustment is required when used in combination with CYP3A inhibitors.
Avoid concomitant use of moderate or strong CYP3A inducers. Alternative treatment with weak CYP3A inducing properties should be considered.
No inhibitory effect was observed with fruquintinib on CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 or CYP3A4/5 and no induction was observed with fruquintinib on CYP1A2, CYP2B6, or CYP3A4.
Monitor patients more closely when concomitant use with P-gp and BCRP substrates for any adverse reactions and make appropriate dose adjustments of the concomitant medications when necessary.
Fruquintinib can be used concomitantly with gastric acid reducing agents without any restrictions.
Dosage Available
1 mg: 7 capsules/blister pack, 3 blister packs/box
5 mg: 7 capsules/blister pack, 1 blister pack/box
Forensic classification
P1S1S3
Tazverik®
(HUTCHMED)
Active Ingredients
Tazemetostat
Pharmacological Properties
Tazemetostat is an inhibitor of the methyltransferase, enhancer of zeste homolog 2 (EZH2), and some EZH2 gain-of-function mutations including Y646X, A682G, and A692V. Tazemetostat suppressed proliferation of B-cell lymphoma cell lines in vitro and demonstrated antitumor activity in a mouse xenograft model of B-cell lymphoma with or without EZH2 gain-of-function mutations. Tazemetostat demonstrated greater effects on the inhibition of proliferation of lymphoma cell lines with mutant EZH2.
Indication
TAZVERIK is indicated for the treatment of adult patients with relapsed or refractory (R/R) follicular lymphoma (FL) whose tumors are positive for an EZH2 mutation and who have received at least 2 prior systemic therapies.
Dosage Form and Strengths
Each tablet contains 200mg tazemetostat equivalent to 228.3mg tazemetostat hydrobromide.
Tablets: 200 mg film-coated, red, round, biconvex shape and debossed with “EZM 200” on one side and plain on the other.
Dosage Administration
The recommended dosage of TAZVERIK is 800 mg orally twice daily with or without food until disease progression or unacceptable toxicity.
Swallow tablets whole. Do not cut, crush, or chew tablets.
Do not take an additional dose if a dose is missed or vomiting occurs after TAZVERIK, but continue with the next scheduled dose.
Contraindications
None
Adverse Reactions
Serious adverse reactions in ≥2% of patients who received TAZVERIK were general physical health deterioration, abdominal pain, pneumonia, sepsis, and anemia. The most common adverse reactions (≥20%) were fatigue, upper respiratory tract infection, musculoskeletal pain, nausea, and abdominal pain.
Drug Interactions
Avoid coadministration of strong or moderate CYP3A inhibitors with TAZVERIK. If coadministration of moderate CYP3A inhibitors cannot be avoided, reduce TAZVERIK dose.
Avoid coadministration of moderate and strong CYP3A inducers with TAZVERIK.
Coadministration of TAZVERIK with CYP3A substrates, including hormonal contraceptives, can result in decreased concentrations and reduced efficacy of CYP3A substrates.
Dosage Available
Bottles of 240 tablets with a desiccant.
Forensic classification
P1S1S3