Prior art

The most relevant prior art for US patent 12083103B2, "Tacrolimus for improved treatment of transplant patients," can be identified by reviewing the "Prior art references" section within the authoritative patent text on Google Patents [cite: https://patents.google.com/patent/[US12083103](/patent/US12083103)/en].

Below is a breakdown of key prior art references cited in US12083103B2, along with their publication/filing dates, brief descriptions, and potential anticipation of claims under 35 U.S.C. § 102.

Most Relevant Prior Art for US12083103B2

1. EP-A-0 184 162

• Full Citation: EP-A-0 184 162
• Publication/Filing Date: The patent text mentions the preparation of tacrolimus is described in EP-A-0 184 162. While a specific publication or filing date for this document isn't directly provided in the US12083103B2 text, it is understood to predate the priority date of US12083103B2 (May 30, 2007) as it describes the preparation of the active ingredient itself [cite: https://patents.google.com/patent/US12083103/en].
• Brief Description: This patent describes the preparation of tacrolimus (FK-506), the active pharmaceutical ingredient central to US12083103B2. Tacrolimus is a macrolide compound with immunosuppressive activity, valuable for preventing organ rejection, graft versus host diseases, and autoimmune diseases [cite: https://patents.google.com/patent/US12083103/en].
• Potential Anticipation (35 U.S.C. § 102): EP-A-0 184 162 anticipates the existence and chemical composition of tacrolimus itself. Therefore, any claim in US12083103B2 that merely describes tacrolimus as an active substance, without the specific extended-release formulation, improved pharmacokinetic profile, or method of administration, would be anticipated. This fundamental prior art would prevent claims on the compound per se. However, the claims of US12083103B2 are directed to specific extended-release oral dosage forms and methods of treatment using these forms, which are distinct from the compound's initial preparation.

2. EP-A-0 444 659

• Full Citation: EP-A-0 444 659
• Publication/Filing Date: Similar to EP-A-0 184 162, the specific date is not in the US12083103B2 text but it precedes the priority date of US12083103B2 [cite: https://patents.google.com/patent/US12083103/en].
• Brief Description: This patent discloses analogues of tacrolimus [cite: https://patents.google.com/patent/US12083103/en].
• Potential Anticipation (35 U.S.C. § 102): This reference anticipates the existence of tacrolimus analogues. Similar to the original tacrolimus, claims in US12083103B2 that broadly cover "pharmaceutically active analogue thereof" without specific reference to the extended-release characteristics or improved pharmacokinetic profiles, would be anticipated. The novelty of US12083103B2 lies in the formulation and method, not in the basic chemical structure of the active compounds.

3. U.S. Pat. No. 6,387,918

• Full Citation: U.S. Pat. No. 6,387,918
• Publication/Filing Date: The US12083103B2 text does not specify the publication/filing date. However, being a granted US patent, its filing date would precede its grant date. It is cited for disclosing analogues of tacrolimus [cite: https://patents.google.com/patent/US12083103/en].
• Brief Description: This patent, like EP-A-0 444 659, discloses analogues of tacrolimus [cite: https://patents.google.com/patent/US12083103/en].
• Potential Anticipation (35 U.S.C. § 102): Similar to the European analogue patent, this US patent anticipates the existence of various tacrolimus analogues. Claims in US12083103B2 concerning the broad use of tacrolimus analogues, absent the specific extended-release features, may be anticipated.

4. WO99/49863

• Full Citation: WO99/49863
• Publication/Filing Date: The US12083103B2 patent refers to WO99/49863 in the context of Prograf®. The "fast release conventional product Prograf® comprises tacrolimus in a physical mixture of HPMC, lactose, cross carmellose sodium as described in Example 31 in WO99/49863". The "99" in WO99 indicates a 1999 filing year for this PCT application [cite: https://patents.google.com/patent/US12083103/en].
• Brief Description: This patent describes formulations of tacrolimus, specifically the conventional, fast-release product Prograf®, which includes tacrolimus in a physical mixture with excipients like HPMC, lactose, and croscarmellose sodium [cite: https://patents.google.com/patent/US12083103/en].
• Potential Anticipation (35 U.S.C. § 102): WO99/49863 is highly relevant as it describes conventional tacrolimus formulations (Prograf®). It anticipates claims relating to tacrolimus compositions that do not exhibit the extended-release profile or improved pharmacokinetic parameters as defined in US12083103B2. Specifically, Claims 1, 11, and 15 of US12083103B2 differentiate themselves by the "extended release oral dosage form" with a specific dissolution profile, the "conversion" to such a form with a reduced dose, and the "initial treatment" with an extended-release form providing specific systemic exposure. WO99/49863, describing a fast release product, would not anticipate these specific extended-release and pharmacokinetic improvements.

5. WO 2005/020993 and WO 2005/020994

• Full Citation: WO 2005/020993 and WO 2005/020994
• Publication/Filing Date: These are patent applications by the present inventors and relate to tacrolimus compositions, indicating a filing year of 2005, prior to the priority date of US12083103B2 [cite: https://patents.google.com/patent/US12083103/en].
• Brief Description: WO 2005/020993 tested different tacrolimus formulations (fast and slow release) showing improved bioavailability compared to Prograf®. WO 2005/020994 relates to solid dispersions comprising tacrolimus, linking improved bioavailability to having tacrolimus in a dissolved state in the dosage form [cite: https://patents.google.com/patent/US12083103/en].
• Potential Anticipation (35 U.S.C. § 102): These references are highly relevant as they are from the same inventors and discuss improved bioavailability and extended-release formulations of tacrolimus. They could potentially anticipate aspects of US12083103B2 that broadly cover extended-release tacrolimus or improved bioavailability. However, US12083103B2 claims specific dissolution profiles (e.g., at most 63.5% release at 12 hours) and specific pharmacokinetic improvements (e.g., reduced Cmax, increased AUC, specific conversion ratios, and initial treatment parameters for de novo patients) which might be more specific than what is explicitly disclosed or enabled in these earlier applications by the same inventors. The key distinction would lie in whether the specific parameters of the claims in US12083103B2 are taught or rendered obvious by WO 2005/020993 and WO 2005/020994. Given that they are by the same inventors, the later patent (US12083103B2) would likely build upon and differentiate from these earlier works by claiming more specific and advantageous embodiments.