osimertinib 80mg

Product Name: Osimertinib

English Name: Osimertinib

Specification: 80 mg × 30 tablets/box

Manufacturer: Drug International Pharma

[Indications]

Osimertinib is a kinase inhibitor indicated for:

1. Adjuvant therapy after tumor resection in patients with non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test.

2. First-line treatment of patients with metastatic NSCLC whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test.

3. Treatment of patients with metastatic EGFR T790M mutation-positive NSCLC, as detected by an FDA-approved test, who have progressed on or after EGFR TKI therapy.

[Recommended Dosage]

Adjuvant therapy for early-stage NSCLC: 80 mg orally once daily, with or without food, until disease recurrence, occurrence of intolerable toxicity, or for up to 3 years.

Metastatic NSCLC: 80 mg orally once daily until disease progression or occurrence of intolerable toxicity.

[Adverse Reactions]

The most common (>20%) adverse reactions, including laboratory abnormalities, are leukopenia, lymphopenia, thrombocytopenia, diarrhea, anemia, rash, musculoskeletal pain, nail toxicity, neutropenia, dry skin, stomatitis, fatigue, and cough.

[Administration]

The recommended dosage of Osimertinib is one 80 mg tablet orally once daily, with or without food.

For patients receiving adjuvant therapy, continue treatment until disease recurrence, occurrence of unacceptable toxicity, or for up to 3 years.

For patients with metastatic lung cancer, continue treatment until disease progression or occurrence of unacceptable toxicity. For patients who have difficulty swallowing solid foods:

1) Disperse the tablet in 60 mL (2 ounces) of non-carbonated water. Stir until the tablet disperses into small fragments (the tablet will not dissolve completely), and swallow immediately. Do not crush, heat, or sonicate the tablet during preparation. Rinse the container with 120 mL to 240 mL (4 to 8 ounces) of water, and drink immediately.

2) If administration via a nasogastric tube is required, disperse the tablet in 15 mL of non-carbonated water as described above, then use an additional 15 mL of water to transfer the residue into a syringe. Administer the liquid according to the nasogastric tube instructions, and follow with an appropriate water flush (approximately 30 mL).

What are the differences between Osimertinib and drugs such as Amivantamab and Furmonertinib? Osimertinib, Almonertinib, Furmonertinib, Befotertinib, Rezetinib, and Reertertini—all are third-generation EGFR-TKIs (Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors). They are primarily used to treat non-small cell lung cancer (NSCLC) harboring EGFR-sensitizing mutations (such as 19del and L858R) as well as the T790M resistance mutation. While they share the same core target, key differences exist regarding their development background, clinical data, approved indications, administration methods, resistance profiles, safety profiles, and drug interactions. The following is a summary of these core distinctions:

I. Core Basic Information and Approved Indications

Osimertinib: Original Innovator Drug (AstraZeneca)

Core Approved Indications: The world's first third-generation EGFR-TKI

1. First-line treatment for advanced NSCLC with EGFR-sensitizing mutations;

2. Second-line treatment for advanced NSCLC with the T790M mutation;

3. Postoperative adjuvant treatment for early-stage NSCLC.

Almonertinib: Domestic Original Innovator Drug (Hengrui Medicine)

Core Approved Indications: China's first third-generation EGFR-TKI

1. Second-line treatment for advanced NSCLC with the T790M mutation;

2. First-line treatment for advanced NSCLC with EGFR-sensitizing mutations.

Furmonertinib: Domestic Original Innovator Drug (Allist Pharmaceuticals)

Core Approved Indications: 1. Second-line treatment for advanced NSCLC with the T790M mutation;

2. First-line treatment for advanced NSCLC with EGFR-sensitizing mutations.

Befotertinib: Domestic Original Innovator Drug (Betta Pharmaceuticals)

Core Approved Indications: Second-line treatment for advanced NSCLC with the T790M mutation.

Rezetinib: Domestic Original Innovator Drug (Chia Tai Tianqing)

Core Approved Indications: Second-line treatment for advanced NSCLC with the T790M mutation.

Reertertini: Domestic Original Innovator Drug (Kelun Pharmaceutical)

Core Approved Indications: Second-line treatment for advanced NSCLC with the T790M mutation.

II. Key Clinical and Administration Differences

1. **Route of Administration and Dosage**

**Osimertinib:** Oral administration, 80 mg once daily; this is the recommended dosage for first-line treatment.

**Ametinib:** Oral administration, 110 mg once daily; this is also the recommended dosage for first-line treatment.

**Furmonertinib:** Oral administration, 80 mg once daily; this is also the recommended dosage for first-line treatment.

**Befotertinib / Rezetinib / Reerertinib:** In their currently approved second-line treatment indications, the dosage regimens vary (e.g., Befotertinib is 80 mg twice daily); all are administered orally once or twice daily, and no intravenous formulations are available.

**2. Status in First-Line Treatment**

**Osimertinib:** The global and domestic "gold standard" for first-line treatment. Based on the FLAURA study, it significantly extends both progression-free survival (PFS) and overall survival (OS). Furthermore, it is the only third-generation EGFR-TKI approved for the adjuvant treatment of early-stage lung cancer.

**Ametinib / Furmonertinib:** The first domestically developed third-generation EGFR-TKIs to receive approval for first-line treatment. Official claims—based on clinical studies conducted in the Chinese population—suggest their efficacy is non-inferior to that of Osimertinib; however, in practice, their efficacy tends to be slightly lower. Nevertheless, they remain important options for first-line treatment within China.

**Befotertinib / Rezetinib / Reerertinib:** Currently approved only for second-line treatment (specifically for patients with the T790M mutation) and have not yet received approval for first-line treatment indications.

**3. Mechanisms of Resistance and Subsequent Treatment**

**Osimertinib:** The most common mechanism of resistance is the C797S mutation; other mechanisms include MET amplification, HER2 amplification, etc. Upon the development of resistance, genetic testing is required to guide the selection of subsequent treatment strategies (e.g., chemotherapy, combination therapy with anti-angiogenic agents, participation in clinical trials for fourth-generation EGFR-TKIs, etc.).

**Domestically Developed Third-Generation EGFR-TKIs (Ametinib / Furmonertinib / Befotertinib / Rezetinib / Reerertinib):** Their resistance profiles are similar to that of Osimertinib; however, some of these agents exhibit varying inhibitory activity against specific rare mutations (e.g., G79X). Additionally, the accumulated clinical data for these agents covers a shorter timeframe compared to that of Osimertinib. 4. Safety Profile

Third-generation EGFR-TKIs generally demonstrate a favorable safety profile. Common adverse reactions primarily include rash, diarrhea, paronychia, interstitial lung disease (ILD), QT interval prolongation, and thrombocytopenia; the key differences lie in their incidence rates and severity:

Osimertinib: Exhibits a low incidence of ILD (approximately 1%), moderate rates of rash and diarrhea, and overall good tolerability.

Ametinib: Characterized by relatively low incidence rates of rash and diarrhea, and minimal impact on the cardiac QT interval.

Furmonertinib: Demonstrates superior activity against rare mutations, a low incidence of ILD, and a more favorable overall safety profile.

Befotnib and other second-line domestic agents: Due to specific dosing regimens, some of these drugs present slightly higher incidence rates of gastrointestinal and dermatological toxicities—such as diarrhea and rash—necessitating individualized patient monitoring.

5. Drug Interactions

Osimertinib: Metabolized via CYP3A4; dose adjustments are required when co-administered with strong CYP3A inhibitors or inducers, and its drug interaction profile is relatively well-defined.

Domestic Third-Generation Agents: Exhibit slightly different metabolic pathways (e.g., some are metabolized via CYP2D6); when co-administered with chemotherapy agents, antifungals, or anti-tuberculosis medications, they carry a lower risk of drug interactions, making them particularly suitable for patients with underlying comorbidities or those requiring polypharmacy.

6. Drug Accessibility and Insurance Coverage

Osimertinib: An originator drug with extensive insurance coverage, having been included in the National Reimbursement Drug List; generic versions are also available on the market at lower price points.

Ametinib / Furmonertinib: Domestic originator drugs that have both been included in the national insurance scheme; they offer high cost-effectiveness and represent mainstream clinical choices within the domestic market.

Befotnib / Rezetinib / Reeratinib: Domestic originator drugs approved more recently; their insurance coverage and clinical application scenarios remain relatively limited, serving primarily as supplementary options within second-line treatment regimens. III. Summary

Osimertinib: Possesses the most mature global clinical data and the most comprehensive range of indications (first-line, second-line, and adjuvant therapy). It serves as a core medication for both advanced and early-stage EGFR-mutated lung cancer, backed by the highest level of evidence regarding safety and efficacy.

Ametinib and Furmonertinib: Represent the core choices for first-line treatment among domestically produced third-generation drugs. Their efficacy is comparable to that of Osimertinib. As purely domestic products, they are the primary recommendations for the general public in local Chinese hospitals (whereas Osimertinib is typically recommended for elite groups and civil servants). With comprehensive coverage under the national medical insurance system, they are highly suitable for the first-line treatment of Chinese patients.

Befotertinib, Rezetinib, and Reerertinib: Primarily utilized for the second-line treatment of T790M-mutated cancers, serving as supplements to the existing range of domestically produced second- and third-generation drugs. Their clinical application scenarios remain relatively limited, and data regarding their safety and efficacy still require verification through long-term follow-up studies.

Manufacturer Profile:

Drug International Ltd (DIL) is a long-established pharmaceutical company based in Bangladesh. It stands as the largest pharmaceutical enterprise and a key national industry leader within the country. Founded in 1980 by Dr. M.M. Amjad Hussain, DIL emerged during an era when Bangladesh’s economy was underdeveloped and poverty was widespread. Since its inception, the company has operated with a low-profile, cost-effective approach, making immense contributions to the health and well-being of countless Bangladeshi citizens. Driven by this corporate ethos—dedicated to benefiting both the nation and its people—DIL rose to become the third-largest manufacturer of pharmaceutical raw materials in Bangladesh by 1997. The company has consistently ranked among Bangladesh's most renowned pharmaceutical firms and serves as a strategic partner to Novartis, one of the world's top three pharmaceutical giants. The DIL Group encompasses a diverse portfolio of subsidiaries, including three large-scale pharmaceutical manufacturing plants, a biopharmaceuticals facility, a health supplements factory, an R&D center for anti-cancer drugs, the Khwaja Yunus Ali Medical College, tea plantations, garment manufacturing operations, ceramics production, printing facilities, and a software development firm. Operating in over 70 countries worldwide, the Group’s product line spans everything from medical devices to a wide array of finished pharmaceutical products, currently comprising a catalog of more than 500 distinct medications.