JAK Inhibitor Formulation and Delivery for Alopecia Areata Treatment

Treating alopecia areata with selective JAK1 inhibitor upadacitinib through oral administration of 30 mg or 15 mg once daily. The treatment achieves significant hair regrowth with minimal side effects, particularly in patients with moderate to severe alopecia areata. The regimen demonstrates rapid improvement in alopecia areata severity, with hair regrowth rates comparable to those achieved with systemic corticosteroids.

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Topical formulations of (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or its salt, for treating skin disorders. The formulations contain a therapeutically effective amount of the compound, which is formulated in an oil-in-water emulsion with a hardener component. The formulation provides stable and easily applied formulations of JAK inhibitors with good skin penetration properties.

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Pharmaceutical composition for preventing and treating JAKs-dominated skin diseases like alopecia areata with reduced resistance and side effects compared to JAK inhibitors alone. The composition combines a JAK inhibitor with cedarwood alcohol (CE), a natural compound with anti-inflammatory and hair growth properties. The CE+JAK inhibitor combination shows enhanced therapeutic effect in mouse models of alopecia areata compared to either alone. It also improves hair growth and reduces hair loss. The synergistic effect suggests CE potentiates JAK inhibition and provides added benefits. The CE+JAK composition could be a better treatment option for skin diseases like alopecia areata with reduced resistance and side effects compared to JAK inhibitors alone.

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A novel treatment for alopecia areata that combines a specific compound with an additional therapeutic agent. The compound targets Janus Kinase 1 and 2, and when combined with a standard treatment regimen, significantly enhances efficacy. The treatment regimen involves administering the compound at a standard dose, followed by a gradual reduction in the compound dose over 8-24 weeks, while maintaining the standard treatment regimen. This dual approach enables sustained hair growth while addressing the underlying autoimmune mechanisms of alopecia areata.

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Selective JAK1 and JAK2 inhibitors for treating autoimmune diseases and inflammatory conditions. The inhibitors target specific JAK enzymes, with the compound of interest being a novel JAK1 and JAK2 inhibitor. This compound has demonstrated therapeutic activity in treating alopecia areata, myelofibrosis, polycythemia vera, alopecia areata, and graft-versus-host disease, among other autoimmune and inflammatory conditions. The compound's mechanism of action involves selective inhibition of JAK1 and JAK2 enzymes, with the potential to modulate JAK activity in a manner distinct from conventional JAK inhibitors.

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A compound that modulates Janus Kinase 1 and 2 activity to treat hair loss disorders like alopecia areata. The compound, represented by a structural formula, is administered as a pharmaceutical salt in a dosing regimen that includes a 24-week initial treatment period followed by a 8-week maintenance phase. The compound's effectiveness in inducing hair growth has been demonstrated in clinical trials.

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A treatment for hair loss conditions like alopecia areata that utilizes a novel compound with therapeutic properties. The treatment involves administering the compound, which modulates Janus kinase activity, particularly JAK1 and JAK2, to promote hair growth. The compound's effectiveness in inducing hair growth has been demonstrated through clinical trials, with measurable improvements in hair density and hair thickness. The treatment can be administered orally in a single dose or divided doses, with dosages ranging from 4-50 mg per day.

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A pharmaceutical agent for treating hair loss disorders like alopecia areata, which improves the SALT score by up to 70% after a single treatment period. The agent, a deuterated analog of a specific kinase inhibitor, specifically targets Janus-Associated Kinase 1 and 2, and when administered at a daily dose of 4-50 mg, exhibits significant hair growth effects. The treatment regimen can be tailored to achieve optimal hair growth while maintaining therapeutic efficacy.

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Treatment of alopecia areata through a novel combination of JAK1/2 inhibitors and a specific compound that modulates these kinases. The treatment involves administering the compound at a daily dose of 8-32 mg, with a 24-week treatment period followed by a 8-week maintenance phase. The compound's mechanism of action is characterized by its selective inhibition of JAK1 and JAK2, which are critical for the pathogenesis of alopecia areata. This treatment approach has shown significant efficacy in inducing hair growth and improving SALT scores in patients with alopecia areata, with clinical improvements of up to 90% in SALT scores.

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Topical formulations for treating inflammatory skin diseases, particularly autoimmune and inflammatory conditions, that combine a JAK1/2 inhibitor with an organic amine pH adjuster. The formulation utilizes a pH-adjusting agent like trolamine, which enables enhanced solubility of the JAK1/2 inhibitor in formulations at pH levels above 4. The pH-adjusting agent can be combined with other formulation components like water, emulsifiers, and solvents to create the desired formulation. The pH-adjusting agent can be independently selected from various amine compounds, including trolamine, ethanolamine, and others. This formulation provides improved solubility and stability of the JAK1/2 inhibitor at pH levels above 4, enhancing its therapeutic efficacy in inflammatory skin diseases.

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Selective JAK1 and JAK2 inhibitors with improved pharmacokinetics and therapeutic efficacy for autoimmune and inflammatory conditions. The compounds, represented by Formula (I), exhibit enhanced activity compared to existing JAK inhibitors, particularly in hair loss disorders like alopecia areata. These selective JAK inhibitors can be combined with conventional JAK inhibitors to form therapeutic formulations that provide potent anti-inflammatory and immunosuppressive effects. The compounds' improved pharmacokinetics enable more sustained therapeutic activity in the treatment of alopecia areata and other autoimmune diseases.

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A topical formulation of tofacitinib for treating skin conditions like alopecia areata, vitiligo, and psoriasis. The formulation combines tofacitinib with a proprietary matrix that enhances its stability and skin tolerance compared to existing oral formulations. The matrix formulation delivers the active drug in a controlled, sustained release that minimizes systemic side effects while maintaining effective skin penetration.

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A method for inducing hair growth through targeted JAK1 and JAK2 inhibition, specifically for alopecia areata. The treatment involves administering a deuterium-substituted compound like Compound I, which selectively targets JAK1 and JAK2 activity while maintaining normal metabolism. The compound is administered twice daily at a dosage range of 4-50 mg/day, with the dosage optimized for hair growth. This approach enables sustained JAK1 and JAK2 inhibition without significant metabolic side effects, potentially leading to permanent hair regrowth in alopecia areata patients.

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A topical formulation of tofacitinib that enhances skin penetration and retention while maintaining efficacy. The formulation combines tofacitinib citrate with a solvent and additional excipients to create a stable and effective topical delivery system. The formulation achieves superior skin penetration compared to conventional formulations, with retention rates of tofacitinib in the skin exceeding penetration rates into the bloodstream.

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A compound that modulates JAK1 and JAK2 activity by deuterium substitution of hydrogen atoms in a drug molecule, enabling improved efficacy, safety, and tolerability in autoimmune skin disorders like alopecia areata. The compound's structural modifications prevent rapid CYP metabolism and promote biologically active metabolites, while maintaining potent JAK1 and JAK2 inhibition. This approach addresses the fundamental ADME issues of rapid drug clearance and toxic metabolites, offering a novel strategy for treating alopecia areata and other autoimmune skin conditions.

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Pyrrolopyrimidine compound with a specific structure, used in the treatment of diseases mediated by Janus kinase. The compound has a pyrrolopyrimidine core with a specific configuration, and its therapeutic efficacy is demonstrated against Janus kinase-mediated diseases through its pharmacological activity.

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Treatment of hair loss disorders like alopecia areata through targeted inhibition of key signaling pathways involved in hair follicle growth and maintenance. The therapy employs specific inhibitors of the Janus kinase (JAK)/Signal transducer and activator of transcription (STAT) pathway, which plays critical roles in cytokine signaling and cell proliferation. By modulating these pathways, the treatment aims to restore normal hair growth patterns in affected individuals.

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A pharmaceutical composition that modulates Janus-associated kinase 1 (JAK1) and/or Janus-associated kinase 2 (JAK2) activity to treat hair loss disorders. The composition comprises a compound or its salt, with the compound having a specific structural formula, and can be administered topically or orally. The compound's ability to modulate JAK1 and JAK2 activity is achieved through deuterium substitution, which enables controlled and selective inhibition of these kinases. The therapeutic effect is demonstrated through hair growth promotion in patients with alopecia areata.

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Inhibition of the Janus activated kinase-signal transducer and activator of transcription (JAK-STAT) pathway, particularly targeting oncostatin, colony stimulating factor 1 receptor, interleukin 34, and trichophages, to promote hair growth. The therapeutic agents selectively target specific components of the JAK-STAT pathway involved in hair follicle regeneration, particularly CSF1R and trichophages, which are known to promote hair growth. These agents can be administered topically to induce hair growth in conditions characterized by hair follicle miniaturization or immune dysfunction.

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Treatment of hair loss disorders through targeted inhibition of cytokine signaling pathways. The treatment involves administering inhibitors of specific protein tyrosine kinases (PTKs) involved in cytokine signaling, such as Jak1, Jak2, and Stat1. These inhibitors can be delivered via various routes, including subcutaneous, intramuscular, intraperitoneal, or intravenous injections, and can be administered daily, weekly, or monthly. The treatment has been found to induce hair growth in patients with hair loss disorders, including alopecia areata, and can also be used to treat hair growth disorders such as hypertrichosis.

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