Trametinib 0.5mg, 2mg Tablets — MEK1/2 Inhibitor for BRAF V600-Mutated Metastatic Melanoma, NSCLC, Anaplastic Thyroid Cancer and Metastatic Solid Tumours
Meqsel® (Trametinib) — MEK Inhibitor for BRAF V600-Mutated Cancers
The First Approved MEK Inhibitor — Transforming Outcomes in BRAF-Mutated Melanoma and Beyond
Meqsel® (Trametinib) is a selective, allosteric MEK1 and MEK2 (mitogen-activated extracellular signal-regulated kinase 1 and 2) inhibitor — used as monotherapy and in combination with Rafinlar (Dabrafenib) for the treatment of BRAF V600E or V600K mutation-positive unresectable or metastatic melanoma, non-small cell lung cancer (NSCLC), anaplastic thyroid cancer (ATC), and other BRAF V600E-mutated solid tumours. Trametinib was the first MEK inhibitor approved for any cancer indication — establishing MEK inhibition as a clinically validated approach to BRAF-driven malignancies.
MEK1 and MEK2 are critical kinases in the RAS/RAF/MEK/ERK mitogen-activated protein kinase (MAPK) signalling pathway — one of the most frequently mutated oncogenic pathways in human cancer. In tumours harbouring BRAF V600 mutations, BRAF is constitutively activated → drives continuous MEK1/2 → ERK activation → uncontrolled tumour cell proliferation and survival. Trametinib inhibits MEK1/2 — blocking this downstream signal and arresting tumour cell growth.
Crucially, Trametinib is most commonly used in combination with Rafinlar (Dabrafenib) — a BRAF inhibitor — creating dual MAPK pathway blockade that overcomes the paradoxical MAPK pathway reactivation that limits single-agent BRAF inhibitor therapy. The Dabrafenib + Trametinib combination has become one of the most important precision oncology regimens across multiple tumour types — with proven survival benefit in melanoma, NSCLC, ATC, and emerging data in other BRAF-mutated solid tumours.
A.K. Pharma is a trusted medicine distributor in Delhi supplying genuine Meqsel (Trametinib) in both 0.5mg and 2mg strengths to hospitals, oncology centres, and pharmacies across India. Manufactured by Novartis India Ltd, Meqsel is available at accessible pricing for Indian patients requiring MEK inhibitor therapy.
What is Meqsel (Trametinib)?
Meqsel contains Trametinib — a highly selective, small molecule allosteric inhibitor of MEK1 and MEK2 kinases. Trametinib binds to an allosteric site on MEK1/2 — adjacent to but distinct from the ATP-binding site — locking MEK in an inactive conformation and preventing both MEK activation by upstream BRAF and MEK-mediated phosphorylation of downstream ERK.
The MAPK Pathway and BRAF V600 Mutations:
The MAPK signalling cascade (RAS → RAF → MEK → ERK) is a fundamental cell proliferation and survival pathway activated by growth factor receptors. In normal cells this pathway is tightly regulated — activated transiently by growth factors and then switched off.
BRAF V600 mutations — most commonly V600E (valine to glutamate substitution at position 600) and V600K — create a constitutively active BRAF kinase that continuously drives MEK → ERK signalling independent of upstream RAS activation. This constitutive MAPK pathway activation:
BRAF V600 mutations occur in:
Why Combination With Dabrafenib Is Superior to Either Agent Alone:
BRAF inhibitors (Dabrafenib) as single agents show impressive initial responses in BRAF-mutated tumours — but resistance develops rapidly (median PFS approximately 5-7 months). A key resistance mechanism is paradoxical MAPK pathway reactivation — BRAF inhibition activates RAS → RAS drives CRAF dimerisation → CRAF drives MEK → ERK reactivation independent of BRAF. Adding MEK inhibition (Trametinib) blocks this downstream reactivation — preventing paradoxical resistance, significantly extending duration of response, and improving OS compared to BRAF inhibitor monotherapy.
Full prescribing information is available at the FDA label for Trametinib.
Clinical Studies and Evidence
METRIC Trial (Trametinib vs Chemotherapy in BRAF V600-Mutated Melanoma) Published in the New England Journal of Medicine (2012), the METRIC trial was the pivotal Phase 3 randomised controlled trial of 322 patients with BRAF V600E or V600K mutation-positive unresectable or metastatic melanoma — comparing Trametinib monotherapy vs chemotherapy (Dacarbazine or Paclitaxel). Key results:
COMBI-d Trial (Dabrafenib + Trametinib vs Dabrafenib Monotherapy in Melanoma) Published in the New England Journal of Medicine (2014) with updated OS data in The Lancet (2016), COMBI-d compared Dabrafenib + Trametinib vs Dabrafenib alone in 423 patients with BRAF V600E/K metastatic melanoma. Key results at 5-year follow-up:
COMBI-v Trial (Dabrafenib + Trametinib vs Vemurafenib in Melanoma) Published in the New England Journal of Medicine (2015), COMBI-v compared Dabrafenib + Trametinib vs Vemurafenib (another BRAF inhibitor) in 704 patients with BRAF V600E/K metastatic melanoma. Key results:
BRF113928 Trial (Dabrafenib + Trametinib in BRAF V600E NSCLC) Published in the New England Journal of Medicine (2017), this Phase 2 trial demonstrated:
BRF117019 Trial (Dabrafenib + Trametinib in Anaplastic Thyroid Cancer) Published in the Journal of Clinical Oncology (2018), this Phase 2 basket study demonstrated:
ROAR and NCI-MATCH Basket Trials (Dabrafenib + Trametinib in Other BRAF V600E Solid Tumours) These tumour-agnostic basket trials demonstrated Dabrafenib + Trametinib activity across multiple BRAF V600E-mutated solid tumours — leading to the first tumour-agnostic approval of this combination for any BRAF V600E-mutated solid tumour after prior therapy.
Available Strengths
Meqsel (Trametinib) is available in the following strengths:
| Presentation | Dose | Use |
|---|---|---|
| Meqsel 0.5mg Tablets | 0.5mg per tablet | Dose reduction — 4 tablets = 2mg (for patients requiring dose reduction) |
| Meqsel 2mg Tablets | 2mg per tablet | Standard dose — 1 tablet daily |
Standard dose: 2mg orally once daily — taken consistently at the same time each day.
Storage — Critical: Meqsel tablets should be stored in a refrigerator at temperatures between 2°C to 8°C and protected from light and moisture. Do not freeze the medication. BioXconomy This is important — Trametinib requires cold chain storage — different from room temperature storage of most oral oncology tablets.
Indications — What Meqsel is Used For
Unresectable or Metastatic Melanoma:
BRAF V600E-Mutated NSCLC:
Anaplastic Thyroid Cancer:
BRAF V600E-Mutated Solid Tumours (Tumour Agnostic):
Important — BRAF V600 Mutation Testing Is Mandatory: Before prescribing Meqsel (Trametinib) for any indication, BRAF V600 mutation status must be confirmed using a validated diagnostic test. BRAF wild-type patients receive no benefit and should not receive BRAF/MEK inhibitor therapy.
For detailed indication information refer to MedlinePlus Trametinib.
Key Benefits of Meqsel
First-in-Class MEK Inhibitor — Validated Precision Oncology Target Trametinib was the first MEK inhibitor approved for any cancer — establishing MEK1/2 inhibition as a clinically proven approach to BRAF-driven malignancies. The METRIC trial demonstrated superior outcomes vs chemotherapy in a randomised trial — proving single-agent MEK inhibition is clinically meaningful in BRAF-mutated melanoma.
Synergistic Combination With Dabrafenib — Dual MAPK Blockade The Dabrafenib + Trametinib combination achieves simultaneous BRAF and MEK inhibition — addressing both the primary oncogenic driver (BRAF V600) and the paradoxical reactivation resistance mechanism (CRAF-driven MEK activation). This dual blockade translates to significantly longer PFS and OS compared to BRAF inhibitor monotherapy — with 19% 5-year PFS in the COMBI-d trial representing durable long-term disease control in a significant proportion of metastatic melanoma patients.
Transformative Activity in Anaplastic Thyroid Cancer ATC historically had median survival of 3-5 months with no effective systemic therapy. Dabrafenib + Trametinib achieved 69% ORR and 14.5-month median OS in BRAF V600E ATC — representing a paradigm shift in the management of this previously rapidly fatal cancer.
Tumour-Agnostic Activity — Applicable Across Multiple BRAF V600E-Mutated Cancers The tumour-agnostic approval of Dabrafenib + Trametinib for any BRAF V600E-mutated solid tumour reflects the fundamental oncogene-driven nature of BRAF V600 signalling — the same mutation driving the same pathway in melanoma, lung cancer, thyroid cancer, colorectal cancer, and glioma all respond to the same targeted combination.
Reduced Cutaneous Toxicity vs BRAF Inhibitor Monotherapy BRAF inhibitors as monotherapy cause paradoxical ERK activation in RAS wild-type keratinocytes → cutaneous squamous cell carcinoma (cuSCC) and keratoacanthoma in 15-20% of patients. Adding Trametinib (MEK inhibitor) blocks this paradoxical ERK activation in skin → dramatically reduces cuSCC from 15-20% to <1% — an important safety benefit of the combination over BRAF inhibitor monotherapy.
Both Strengths Available — Complete Dose Management A.K. Pharma supplies both 0.5mg and 2mg Trametinib — enabling the standard 2mg dose and dose reductions to 1.5mg (three 0.5mg tablets) when required for toxicity management.
How Meqsel Works — MEK Inhibition in BRAF-Mutated Cancers
The Normal MAPK Pathway: Growth factor → receptor tyrosine kinase activation → RAS activation → RAF activation → MEK1/2 phosphorylation and activation → ERK1/2 phosphorylation and activation → ERK translocates to nucleus → transcription factors activated → proliferation genes expressed → cell cycle progression.
BRAF V600 Mutation — Constitutive Activation: BRAF V600E/K mutation → constitutively active BRAF kinase → continuously phosphorylates and activates MEK1/2 → continuous ERK activation → continuous transcription of proliferation genes → uncontrolled tumour cell growth — independent of growth factor input.
Trametinib’s Mechanism:
Step 1 — Allosteric MEK1/2 Binding: Trametinib binds to an allosteric site on MEK1 and MEK2 — adjacent to the kinase domain but distinct from the ATP-binding site. This allosteric binding locks MEK in an inactive conformation — preventing both upstream BRAF-mediated MEK activation and MEK-mediated ERK phosphorylation simultaneously.
Step 2 — ERK Phosphorylation Blockade: Without MEK1/2 activity, ERK1/2 cannot be phosphorylated → inactive ERK cannot translocate to the nucleus → ERK target transcription factors (ETS, AP-1 family) are not activated → proliferation gene expression is suppressed.
Step 3 — Cell Cycle Arrest and Apoptosis: Suppression of ERK-driven transcription leads to reduced cyclin D1 expression → CDK4/6 inhibition → Rb hypophosphorylation → G1 cell cycle arrest. Simultaneously, ERK suppression reduces anti-apoptotic BCL-2 family protein expression → increased apoptosis sensitivity.
Why Combination Dabrafenib + Trametinib is Superior:
BRAF inhibitor monotherapy initially blocks BRAF V600 → ERK → tumour response. However:
For detailed mechanism overview refer to ESMO Melanoma Guidelines and NCCN Melanoma Guidelines.
Meqsel + Rafinlar — The Dabrafenib + Trametinib Combination Regimen
At A.K. Pharma both components of the Dabrafenib + Trametinib combination are available:
| Medicine | Brand | Dose | Available at A.K. Pharma |
|---|---|---|---|
| Trametinib (MEK inhibitor) | Meqsel | 2mg orally once daily | Request Quote |
| Dabrafenib (BRAF inhibitor) | Rafinlar | 150mg orally twice daily | Request Quote |
Standard Combination Dosing:
Tumour Types and BRAF Testing Required:
| Indication | BRAF Mutation | Regimen |
|---|---|---|
| Unresectable/Metastatic Melanoma | V600E or V600K | Dabrafenib + Trametinib (preferred) or Trametinib monotherapy |
| Metastatic NSCLC | V600E only | Dabrafenib + Trametinib |
| Anaplastic Thyroid Cancer | V600E only | Dabrafenib + Trametinib |
| Solid Tumours (tumour agnostic) | V600E only | Dabrafenib + Trametinib |
Dosage and Administration
Trametinib (Meqsel) Standard Dose:
When Used With Dabrafenib:
Dose Reduction for Toxicity:
Important Storage Reminder: Trametinib tablets must be stored in a refrigerator between 2°C and 8°C — take out of refrigerator just before administration. Do not leave at room temperature for extended periods.
Monitoring:
Full dosing guidelines available at Drugs.com Trametinib Dosage.
BRAF V600 Mutation Testing — Essential Before Prescribing
Meqsel (Trametinib) must only be used in patients with confirmed BRAF V600 mutation. Testing options:
CDSCO-approved BRAF V600 testing is available at major cancer centres across India. Re-biopsy of metastatic lesions may be required if the primary tumour biopsy tested negative — tumour heterogeneity and clonal evolution can result in BRAF V600 mutations being present in metastatic deposits but absent in the primary.
Who Should Use Meqsel
Meqsel (Trametinib) is prescribed for:
Melanoma:
NSCLC:
Anaplastic Thyroid Cancer:
Other BRAF V600E-Mutated Solid Tumours:
Meqsel is prescribed by medical oncologists, dermatologists (for melanoma), thoracic oncologists, and endocrinologists/thyroid cancer specialists. A.K. Pharma supplies Meqsel to hospitals, oncology centres, and pharmacies across Delhi and India.
Possible Side Effects
Common side effects of Trametinib monotherapy include rash (57%), diarrhoea (43%), lymphoedema (32%), acneiform dermatitis (19%), peripheral oedema (26%), fatigue (26%), and nausea (26%).
When used in combination with Dabrafenib — side effect profile changes — some Trametinib-specific toxicities (rash) are reduced while Dabrafenib-specific toxicities (fever, fatigue, arthralgias) are added. The combination’s overall tolerability is generally better than expected from combining two targeted therapies.
Serious side effects include:
Cardiomyopathy/Decreased LVEF: Trametinib can cause cardiomyopathy and decreased LVEF — occurring in approximately 7-11% of patients. Monitor LVEF at baseline, 1 month, and every 2-3 months. Withhold for asymptomatic decrease ≥10% from baseline and to below institutional lower limit of normal. Permanently discontinue for symptomatic CHF or persistent LVEF decrease.
Retinal Pigment Epithelial Detachment (RPED): Blurred vision, visual changes, and photopsia may indicate RPED — a serious ocular complication requiring ophthalmological evaluation and treatment interruption.
Interstitial Lung Disease (ILD)/Pneumonitis: Serious ILD occurs in approximately 2% — monitor for new respiratory symptoms; withhold pending evaluation; permanently discontinue for confirmed Grade 3-4 ILD.
Serious Skin Toxicity: Erythema multiforme, Stevens-Johnson syndrome, and drug reaction with eosinophilia and systemic symptoms (DRESS) — rare but serious; permanently discontinue.
Haemorrhage: Serious haemorrhagic events including intracranial and gastrointestinal haemorrhage — permanently discontinue for life-threatening bleeding.
Venous Thromboembolism: DVT and PE — monitor throughout treatment.
Hyperglycaemia: Particularly when combined with Dabrafenib — monitor blood glucose; manage with anti-diabetic therapy as needed.
Full side effect information available at FDA Trametinib Safety Information.
Precautions
Storage and Handling
As a responsible medicine distributor in Delhi, A.K. Pharma maintains full cold chain requirements during storage and supply of Meqsel ensuring product integrity for every unit supplied. Cold chain maintenance for an oral tablet is unusual — confirm cold storage arrangements with the dispensing pharmacy.
Manufacturer Information
Meqsel (Trametinib) is manufactured by Novartis India Ltd — the Indian subsidiary of Novartis AG, a global pharmaceutical leader. Trametinib received FDA approval in May 2013 as the first MEK inhibitor approved for any cancer indication — for unresectable or metastatic melanoma. A.K. Pharma supplies only genuine Meqsel sourced from authorized Novartis distributors.
Related Cancer Medicines Available at A.K. Pharma
Frequently Asked Questions
Q. What is Meqsel used for? Meqsel (Trametinib) is used to treat BRAF V600E or V600K mutation-positive unresectable or metastatic melanoma — as monotherapy or in combination with Rafinlar (Dabrafenib). It is also used in combination with Dabrafenib for BRAF V600E-mutated NSCLC, anaplastic thyroid cancer, and other BRAF V600E-mutated solid tumours. More information available at MedlinePlus.
Q. What is the generic name of Meqsel? The generic name of Meqsel is Trametinib. It is a selective MEK1/2 inhibitor — the first approved MEK inhibitor for cancer treatment — manufactured by Novartis India Ltd.
Q. Is BRAF testing required before taking Meqsel? Yes — BRAF V600 mutation testing is mandatory before prescribing Meqsel. Only patients with confirmed BRAF V600E or V600K mutations should receive Trametinib. BRAF wild-type patients receive no benefit and should not be treated. Testing is available at major cancer centres across India using PCR, NGS, or IHC methods.
Q. Why is Meqsel usually used with Rafinlar (Dabrafenib)? Trametinib monotherapy shows activity in BRAF V600-mutated melanoma but resistance develops due to paradoxical MAPK pathway reactivation through CRAF. Combining with Dabrafenib (BRAF inhibitor) blocks this resistance mechanism — providing dual MAPK pathway suppression that translates to significantly better PFS and OS. The combination also reduces Dabrafenib-associated cutaneous squamous cell carcinoma from 15-20% to <1%.
Q. Does Meqsel need to be stored in a fridge? Yes — unlike most oral cancer tablets, Trametinib requires refrigeration between 2°C and 8°C. Do not freeze. This is an important point for patients and pharmacies. A.K. Pharma maintains cold chain storage for Meqsel throughout storage and supply.
Q. What are the two strengths of Meqsel and how are they used? Meqsel 2mg is the standard dose — one 2mg tablet once daily. Meqsel 0.5mg is the dose reduction strength — used when patients require dose reduction due to toxicity (1.5mg = three 0.5mg tablets; 1.0mg = two 0.5mg tablets). A.K. Pharma supplies both strengths for complete dose management.
Q. Can Meqsel be used for lung cancer? Yes — in combination with Rafinlar (Dabrafenib) for BRAF V600E mutation-positive metastatic NSCLC. BRAF V600E mutations occur in approximately 2-4% of NSCLC adenocarcinomas. NGS-based comprehensive molecular profiling is recommended for all NSCLC patients to identify actionable mutations including BRAF V600E.
Q. Is Meqsel available in India? Meqsel (Trametinib) can be supplied to hospitals, oncology centres, and pharmacies across India through licensed pharmaceutical distributors. Contact A.K. Pharma — medicine distributor in Delhi — for availability and pricing.
Q. What is the price of Meqsel in India? Meqsel price in India varies by strength and pack size. Contact A.K. Pharma at 011 4172 6999 or WhatsApp +91 9810034827 for current pricing and bulk supply rates.
Q. How to order Meqsel from A.K. Pharma? You can request a quote directly from this page, call us at 011 4172 6999, or WhatsApp us at +91 9810034827 with your requirements and we will respond promptly.
Q. Does A.K. Pharma supply Meqsel in bulk? Yes. A.K. Pharma supplies Meqsel in bulk to oncology centres, hospitals, and pharmacies across Delhi and India with cold chain maintained throughout. Contact us for bulk pricing and availability.
Why Order Meqsel from A.K. Pharma?
Contact A.K. Pharma for Meqsel Supply 📍 E-2/257A, 2nd Floor, Shastri Nagar, New Delhi 110052 📞 011 4172 6999 📱 WhatsApp: +91 9810034827 🌐 akpharma.in