Category Archives: CB-03-01

Update on Breezula (aka CB-03-01)

In 2014, I wrote about a new yet to be released topical antiandrogen product called CB-03-01. Historically, antiandrogen products have usually been ingested orally and often led to adverse side effects. Early reports suggest that topical CB-03-01 has no significant side effects.

In 2015, the Italian company (Cosmo Pharmaceuticals) that was compounding CB-03-01 changed the product’s name to the unusual Breezula.  Moreover, Cosmo itself was renamed as Cassiopea.  I wrote about those developments here.

Phase 2 Results

Yesterday, Cassiopea released an interesting PowerPoint presentation summarizing 2015 and projecting the outlook for 2016.  For us hair loss sufferers, pages 18-22 summarizing Breezula’s Phase 2 Proof of Concept (PoC) results is the most important section.

To summarize in brief:

  • 95 patients were enrolled in a double blind study that lasted for 6 months and ended in December 2015.
  • 31 patients were on Breezula 5%, 31 patients were on Minoxidil 5% and 33 patients were given nothing except a vehicle (i.e., placebo).
  • Of the 95 patients, 78 lasted till the end of the 6-month treatment period, and 73 of those were deemed to have completed the protocol without any violations.  Of those 73 patients, 23 were on Breezula, 25 were on Minoxidil and 25 were on a placebo.  A fairly even distribution.
  • 39 percent of patients on Breezula had at least some improvement in hair growth, compared to 36 percent of those on Minoxidil.  26 percent of patients on Breezula had at least some worsening in hair growth, compared to 16 percent of those on Minoxidil.  Status quo was maintained in 35 percent of Breezula patients versus 48 percent of Minoxidil patients.
  • Later in 2016, Cassiopea will commence further dosing related trials for Breezula.  I wonder if they will compare the effectiveness of higher doses to the effectiveness of the much more rarely used Minoxidil 15%?

I was pleased to see the results. Overall, Breezula seems as good as Minoxidil, and since the latter is not an anti-androgen, we can use both products topically on our scalp for two separate positive effects. Perhaps we can also add topical Bimatoprost and topical Finasteride to that combo later this year, and then we would have a quartet of topical products, each tackling a different mechanism of balding.

Of course Breezula is still years from release (even if we assume they can speed up phase 3 trials like is the case in Japan, with newer regulations), but some people on hair loss forums are purchasing it illegally or even making it at home. I cannot ever recommend that.  An even more optimistic scenario is the addition of Samumed’s topical SM04554 to the mix whenever that comes out.  It would be funny if in 2020, I started applying a quintet of topical products to my scalp and then suddenly a simple cure for hair loss came out that made all those topical products obsolete.

For younger people who have only been balding for a few years or less, such incremental developments are probably not too exciting. For those of us who have been following the hair loss industry for many more years, it is very pleasing to finally see new products arriving.  It is ridiculous that there have only ever been two products officially FDA approved to tackle hair loss — 1) Finasteride and 2) Minoxidil.

***Note that on page 8 of the PowerPoint presentation they have labeled CB-03-01 as “Winlevi” and CB-03-11 as “Breezula”.  Winlevi (for acne) and Breezula (for hair loss) contain the same key antiandrogen ingredient (a steroid belonging to the family of cortexolone derivatives), but in different formulations.

CB-03-01

Due to the numerous news items, conferences and other hair loss research related developments in recent months, I have had to delay covering an important product until today.  This product, as evident from the title of this post, is CB-03-01 (Edit: name changed to Breezula), a topical anti-androgen type molecule that is as yet not approved for sale and is still undergoing clinical trials.

CB-03-01 is manufactured by Italy-based Cosmo Pharmaceuticals (Edit: name changed to Cassiopea), a company that is primarily focused on treating Inflammatory Bowel Diseases (IBD) and colon cancer.  Strangely enough, the company has also been active in the seemingly entirely unrelated skin disorders area. Cosmo licensed the CB-03-01 product to Medicis (US) in early 2012, but Valeant (Canada) then purchased Medicis later in the same year.  Per some reports, Valeant still seems to be interested in the product, although it has an option for right of refusal in case of Cosmo re-licensing.

The CB-03-01 product will supposedly cure (or improve?) acne, hirsutism and male pattern baldness (MPB).  This very useful January 2013 Cosmo Presentation has a number of pages on CB-03-01 for both acne and hair loss applications.  My favorite is the diagram on page 48.  It shows that while Finasteride and Dutasteride work on preventing the conversion from Testosterone to DHT, CB-03-01 does not mess with that perhaps important hormonal mechanism, but rather, acts at the receptor site (in their own words on page 51: “antagonize the DHT/T interaction at these receptors”).

The one discouraging aspect of the above presentation’s page 48 diagram is that it seems to compare CB-03-01’s mechanism of action with that of Cyproterone Acetate and Flutamide, neither of which have turned out to be of any major help for most people when it comes to hair regrowth (and mixed testimonials when it comes for hair maintenance).  Luckily, while those two drugs are taken orally, CB-03-01 will be applied topically and most likely result in far fewer side effects.  Note that CB-03-01 is technically known as Cortexolone 17α-propionate according to this source.

Key Events Affecting CB-03-01 (parts of below directly pasted from their site with my modifications in some places)

  • IND granted in Q1 2012 for acne treatment.
  • Phase II dose escalating clinical trials for acne treatment completed in H1 2014.
  • An FDA meeting for discussion of the phase III acne trial design is expected at the end of 2014 or beginning of 2015.
  • The first patient in for a “proof of concept” phase II trial for alopecia is expected in October 2014.
  • Patents have been granted in the US and expire in 2023 and 2030.

Cosmo’s half-year 2014 report has more recent updates, including a useful clinical trial and schedule of release diagram for all its key products on page 14.

I will probably have more on CB-03-01 in coming posts, as there is a lot of discussion about this on the forums and I have not had much time to process most of it, especially Desmond’s recent thread.