Abbott ordains Elan to marry Tricor and Crestor

In the face of generic competition, Abbott has asked Irish biotechnology firm Elan to use its NanoCrystal technology to develop an "all in one" oral dose formulation combining two cholesterol drugs, AstraZeneca's Crestor and Abbott's Tricor, as demand for combination therapy, now 15 per cent of the cholesterol market, continues to grow.

Cholesterol-lowering drugs are the largest-selling category of drugs in the world but their market, currently valued at $32bn (€25bn) globally, is becoming more generic, as successful drugs such as Merck's Zocor (simvastatin) and Bristol Myers Squibb's Pravachol (pravastine sodium) come off patent, so drugmakers are turning to combined formulations that are more popular with patients because they are cheaper than paying for two prescriptions and are often more effective.

Elan's NanoCrystal technology can be utilised in a combination product to optimise bioavailability and absorption in patients, particularly of poorly water-soluble compounds, making it an attractive choice for Abbott and AstraZeneca, whose Tricor and Crestor respectively both treat adults with high cholesterol.

Although the two dugs are lipid-regulating agents, they belong to a different category of drugs; TriCor, part of a class of medications called fibrates, has been shown to predominately reduce triglycerides and raise high-density lipoprotein (HDL), while Crestor is a statin which predominantly reduces low-density lipoprotein (LDL) cholesterol.

Thus, their combination would potentially address LDL cholesterol, HDL cholesterol and triglycerides simultaneously with a combined fibrate and statin medication in a single pill, leading to improved compliance and outcomes.

Nevertheless, Abbott is also exploring a different combination, that of its next-generation fenofibrate (ABT-335) currently in Phase III clinical trials, and Crestor, a formulation which does not require Elan's technology.

Which of the combinations will be developed further will depend upon data generated from the initial studies and the development costs and profits over the duration of the collaboration will be shared between Abbott and AstraZeneca.

Elan has already worked with Abbott on a new formulation of Tricor which allows for administration with or without food - the old formulation had to be taken with a meal - in a move which in 2004 created a new patent for Tricor and so assisted the drugmaker in its legal struggle to keep the medicine off the hands of generic manufacturers.

Still Abbot is currently engaged in an acrimonious legal battle with generic manufacturers who allege the Illinois company has changed formulations of TriCor so many times, it has violated US antitrust laws, so a combination with Crestor or ABT-335, instead of another reformulation of the same drug, would also help Abbott in that area.

"We are very pleased to execute this agreement, which follows on from the successful application of our NanoCrystal Technology in the current TriCor 145 product," said Paul Breen, Elan's executive vice president.

"We hope applying this technology will result in the successful development and launch of a combination product that will benefit patients."

Many innovative drug candidates are abandoned because of poor pharmacokinetic properties, including absorption, distribution, metabolism, and excretion, giving Elan's NanoCrystal technology an edge.

Since poor water solubility correlates with slow dissolution rate, Elan's formulation approach increases the drug's surface area by reducing particle size, leading to an increase in dissolution rate.

This is accomplished with NanoCrystal particles, which are typically less than 1,000 nanometres in diameter and are produced by milling the drug substance using Elan's wet-milling technique.

The NanoCrystal particles of the drug are stabilized against agglomeration by surface adsorption of selected GRAS (Generally Regarded As Safe) stabilisers, so the result is an aqueous dispersion of the drug substance that behaves like a solution, a NanoCrystal colloidal dispersion, which can be processed into finished dosage forms for all routes of administration.

The technology can be incorporated into all dosage forms, either parenteral and oral, including solid, liquid, fast-melt, pulsed release and controlled release dosage forms.

Under the terms of the its licence agreement with Abbott, Elan will receive payments upon the achievement of development, clinical, and regulatory milestones, as well as royalty payments based on sales of the combination product, if successfully developed and commercialised in the US, something not expected before 2010.

By then generic competition will be even fiercer, so not surprisingly Abbott and AstraZeneca are not the only drug firms to be using combined formulation to prepare for the tough times ahead.

Pfizer, the world's biggest drugmaker, is working on a pill combining its experimental drug torcetrapib, which boosts good cholesterol, with its statin Lipitor, the world's biggest blockbuster which brought in more than $8bn in sales last year, according to research firm IMS Health.

Merck, on the other hand, which last month lost patent protection on the world's second best-selling drug, the statin Zocor, has already formulated Schering-Plough's statin Zetia with Zocor and marketed it under the brand name Vytorin, with sales of this combined drug doubling last year to $2.4bn.

Even if combination pills are a long way from overtaking statin drugs, which generated $16bn in US sales last year according to IMS Health, the fact that the drug's industry's most lucrative sector sees such an interest in combined formulation speaks volumes about the potential of this developmental approach.