New Kaletra tablet formulation (meltrex) approved by FDA

On 28 October 2005, the Food and Drug Administration (FDA) approved a new formulation of Kaletra. Kaletra (lopinavir/ritonavir) is now available in the US as a film-coated tablet (200mg/50mg) that provides advantages over the currently marketed capsule formulation for HIV-1 infected patients. Specifically, the tablet formulation:

  • does not require refrigeration
  • can be administered without regard to meals
  • does not require dose adjustments for concomitant use with certain NNRTIs and PIs in treatment-naive patients
  • has a decreased pill burden compared to the capsule formulation (2 tablets twice daily or 4 tablets once daily in treatment-naive patients only vs 3 capsules twice daily or 6 capsules once daily in treatment-naive patients only)

Selected changes to the SPC for the tablet formulation are included below. Please refer to the full SPC for full details of the changes.

  • Two 200/50 mg lopinavir/r tablets are similar to three 133.3/33.3 mg KALETRA capsules under fed conditions with less pharmacokinetic variability.

No clinically significant changes in Cmax and AUC were observed following administration of lopinavir/r tablets under fed conditions compared to fasted conditions. Relative to fasting, administration of lopinavir/r tablets with a moderate fat meal (500 – 682 Kcal, 23 to 25% calories from fat) increased lopinavir AUC and Cmax by 26.9% and 17.6%, respectively. Relative to fasting, administration of lopinavir/r tablets with a high fat meal (872 Kcal, 56% from fat) increased lopinavir AUC by 18.9%, but not Cmax. Therefore, lopinavir/r tablets may be taken with or without food.

  • Lopinavir/r oral solution must be taken with food.
  • Lopinavir/r tablets should be swallowed whole and not chewed, broken, or crushed.

The ‘dosage and administration’ section was revised to include the following information:

  • Although the label includes an option to dose lopinavir/r once-daily for treatment naive patients, once-daily administration of lopinavir/r is not recommended in therapy-experienced patients.

Drug interactions with the tablet and capsule formulation are similar and require similar dose adjustments.

The ‘how supplied’ section was revised to include storage information for the Kaletra tablets as follows:

  • Recommended storage for the film-coated tablets is at 20°- 25°C (68°-77°F); excursions permitted to 15°-30°C (59° to 86°F) [see USP controlled room temperature]. Exposure of this product to high humidity outside the original container for longer than 2 weeks is not recommended.

Abbott plan to phase out the capsule formulation of lopinavir/r


European approval is not expected until early Summer 2006. However a named patient programme is being planned within the next month, that will enable earlier access for patients who currently have adherence or storage problems associated with the current formulation.

The cost premium in the US for the new formulation was an 8% increase, although this is not expected in Europe. Once the meltrex formulation is available, Abbott will discontinue production of the current formulation.

Source: FDA list serve

Links to other websites are current at date of posting but not maintained.