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


2024-09-23 於2024月09月23日

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

HKPharmJ

Tel: 23763090

Email: editor@hkpj.org

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