Johnson & Johnson has moved a potential successor compound to the antipsychotic Risperdal (risperdone) into Phase III clinical studies.

Paliperidone ER, which is a metabolite of risperdone formulated using the Alza OROS controlled-release technology, entered Phase III for treatment of schizophrenia in February, the company disclosed in an April 13 pipeline update to investors.

J&J has kept quiet about the paliperidone (code-named R-092670) development effort until it reached Phase III. The basic risperidone patent expires in December 2007, making paliperidone a high-priority project for the company. Like risperidone, paliperidone is a dual dopamine D-2 and serotonin 5-HT2 receptor antagonist.

At the time of the Alza acquisition in 1999, J&J highlighted the Risperdal franchise as a candidate to benefit from Alza's drug formulation technologies.

Paliperidone joins another product of the Alza acquisition, dapoxetine for premature ejaculation, to give J&J a total of two new molecular entities in Phase III.

J&J has already launched one new formulation for risperidone, the long-acting injectable Risperdal Consta . The company also has a supplemental application pending for Risperdal as a treatment for autism (filed in December).

J&J believes paliperidone ER will have an improved side effect profile compared to Risperdal.

J&J has at least two ongoing trials of paliperidone in the U.S. The first will evaluate three fixed dosages of extended-release paliperidone (6 mg/day, 9 mg/day and 12 mg/day) versus placebo for six weeks in 595 patients.

During an open-label extension phase, patients will receive add-on therapy with 10 mg/day of olanzapine (Lilly's Zyprexa ). The study is expected to conclude in January 2006.

The second Phase III trial will test paliperidone versus placebo in 440 adults with acute schizophrenia, and is expected to conclude in December.

J&J is also testing an intramuscular injection formulation of paliperidone palmitate in Phase I, and is conducting a Phase II international trial with an unspecified formulation of the drug.

Apart from paliperidone and dapoxetine, J&J's Phase III and registration pipeline consists of line extensions, including additional indications and/or formulations for Topamax (topiramate), Remicade (infliximab), Procrit (epoetin alfa), Levaquin (levofloxacin) and Reopro (abciximab).

One potential line extension, an extended-release formulation of Alzheimer's agent Reminyl , was deemed "not approvable" by FDA in December, J&J disclosed. The company has also discontinued development of Reminyl for mild cognitive disorder.

According to F-D-C Reports' ¹ NDA Pipeline , J&J has another antipsychotic agent in clinical trials: R-209130, which is in Phase II for treatment of negative symptoms of schizophrenia.

- Alla Rutstein Bobbitt

J&amp;J Antipsychotic Paliperidone ER Moves Into Phase III

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J&J Antipsychotic Paliperidone ER Moves Into Phase III