KALETRA Drug Patent Profile

When do Kaletra patents expire, and when can generic versions of Kaletra launch?

Kaletra is a drug marketed by Abbvie and is included in three NDAs.

The generic ingredient in KALETRA is lopinavir; ritonavir. There are thirteen drug master file entries for this compound. Six suppliers are listed for this compound. Additional details are available on the lopinavir; ritonavir profile page.

DrugPatentWatch^® Litigation and Generic Entry Outlook for Kaletra

A generic version of KALETRA was approved as lopinavir; ritonavir by LANNETT CO INC on December 27^th, 2016.

Summary for KALETRA

US Patents:	0
Applicants:	1
NDAs:	3
Finished Product Suppliers / Packagers:	2
Raw Ingredient (Bulk) Api Vendors:	3
Clinical Trials:	152
Drug Prices:	Drug price information for KALETRA
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for KALETRA
What excipients (inactive ingredients) are in KALETRA?	KALETRA excipients list
DailyMed Link:	KALETRA at DailyMed

See drug prices for KALETRA

Recent Clinical Trials for KALETRA

Identify potential brand extensions & 505(b)(2) entrants

Sponsor	Phase
OHSU Knight Cancer Institute	Phase 2
Oregon Health and Science University	Phase 2
October 6 University	Phase 4

See all KALETRA clinical trials

Pharmacology for KALETRA

Drug Class

Cytochrome P450 3A Inhibitor Protease Inhibitor

Mechanism of Action

Breast Cancer Resistance Protein Inhibitors Cytochrome P450 1A2 Inducers Cytochrome P450 2B6 Inducers Cytochrome P450 2C19 Inducers Cytochrome P450 2C9 Inducers Cytochrome P450 2D6 Inhibitors Cytochrome P450 3A Inducers Cytochrome P450 3A Inhibitors Cytochrome P450 3A4 Inhibitors HIV Protease Inhibitors Organic Anion Transporting Polypeptide 1B1 Inhibitors P-Glycoprotein Inhibitors UDP Glucuronosyltransferases Inducers

Paragraph IV (Patent) Challenges for KALETRA

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
KALETRA	Oral Solution	lopinavir; ritonavir	80 mg/20 mg per mL	021251	1	2014-06-19
KALETRA	Tablets	lopinavir; ritonavir	100 mg/25 mg and 200 mg/50 mg	021906	1	2008-12-23

US Patents and Regulatory Information for KALETRA

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Abbvie	KALETRA	lopinavir; ritonavir	CAPSULE;ORAL	021226-001	Sep 15, 2000		DISCN	No	No
Abbvie	KALETRA	lopinavir; ritonavir	TABLET;ORAL	021906-001	Oct 28, 2005	AB	RX	Yes	Yes
Abbvie	KALETRA	lopinavir; ritonavir	SOLUTION;ORAL	021251-001	Sep 15, 2000	AA	RX	Yes	Yes
Abbvie	KALETRA	lopinavir; ritonavir	TABLET;ORAL	021906-002	Nov 9, 2007	AB	RX	Yes	No

Expired US Patents for KALETRA

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Abbvie	KALETRA	lopinavir; ritonavir	TABLET;ORAL	021906-002	Nov 9, 2007	5,674,882*PED
Abbvie	KALETRA	lopinavir; ritonavir	SOLUTION;ORAL	021251-001	Sep 15, 2000	6,284,767*PED
Abbvie	KALETRA	lopinavir; ritonavir	CAPSULE;ORAL	021226-001	Sep 15, 2000	5,914,332*PED
Abbvie	KALETRA	lopinavir; ritonavir	TABLET;ORAL	021906-001	Oct 28, 2005	5,886,036*PED
Abbvie	KALETRA	lopinavir; ritonavir	TABLET;ORAL	021906-002	Nov 9, 2007	5,914,332*PED
Abbvie	KALETRA	lopinavir; ritonavir	SOLUTION;ORAL	021251-001	Sep 15, 2000	5,541,206*PED
Abbvie	KALETRA	lopinavir; ritonavir	SOLUTION;ORAL	021251-001	Sep 15, 2000	8,501,219

EU/EMA Drug Approvals for KALETRA

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Mylan Pharmaceuticals Limited	Lopinavir/Ritonavir Mylan	lopinavir, ritonavir	EMEA/H/C/004025 Lopinavir/ritonavir is indicated in combination with other antiretroviral medicinal products for the treatment of human immunodeficiency virus (HIV-1) infected adults, adolescents and children above the age of 2 years.The choice of lopinavir/ritonavir to treat protease inhibitor experienced HIV-1 infected patients should be based on individual viral resistance testing and treatment history of patients.	Authorised	yes	no	no	2016-01-14
AbbVie Deutschland GmbH Co. KG	Kaletra	lopinavir, ritonavir	EMEA/H/C/000368 Kaletra is indicated in combination with other antiretroviral medicinal products for the treatment of human immunodeficiency virus (HIV-1) infected adults, adolescents and children aged from 14 days and older.The choice of Kaletra to treat protease inhibitor experienced HIV-1 infected patients should be based on individual viral resistance testing and treatment history of patients.	Authorised	no	no	no	2001-03-19

International Patents for KALETRA

See the table below for patents covering KALETRA around the world.

Country	Patent Number	Title	Estimated Expiration
Netherlands	300060
Croatia	P20180999
Italy	1273979	COMPOSTI CHE INIBISCONO PROTEASI RETROVIRALI
Spain	2694073
Chile	2009001844	Forma de dosificacion farmaceutica solida que comprende lopinavir y ritonavir formulados en forma de dispersion solida o solucion solida, un polimero soluble en agua y un tensioactivo con valores de hlb de entre 4 y 10, util en el tratamiento de una infeccion por vih (divisional sol. 393-06).
European Patent Office	0719142
Australia	2856097

Supplementary Protection Certificates for KALETRA

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
0674513	C00674513	Switzerland		PRODUCT NAME: LOPINAVIR UND RITONAVIR; REGISTRATION NO/DATE: IKS 55648 20001213
0674513	C300060	Netherlands		PRODUCT NAME: RITONAVIR, DESGEWENST IN DE VORM VAN EEN FARMACEUTISCH AAN- VAARDBAAR ZOUT OF EEN FARMACEUTISCH AANVAARDBARE ESTER, EN LOPINAVIR; REGISTRATION NO/DATE: EU/1/01/172/001 - EU/1/01/172/003 20010320
0674513	SPC/GB01/044	United Kingdom		PRODUCT NAME: THE COMBINATION OF THE ACTIVE INGREDIENTS RITONAVIR AND LOPINAVIR; REGISTERED: CH 55649 20001213; UK EU/1/01/172/001 20010320; UK EU/1/01/172/002 20010320; UK EU/1/01/172/003 20010320

KALETRA Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for KALETRA (Lopinavir/Ritonavir)

Introduction

KALETRA, a combination of lopinavir and ritonavir, is a protease inhibitor used in the treatment of HIV-1 infection. Since its introduction, the drug has undergone significant developments in formulation, dosing, and market positioning. Here, we will explore the market dynamics and financial trajectory of KALETRA.

Historical Context and FDA Approvals

KALETRA was first approved by the FDA on September 15, 2000, marking a significant milestone in HIV treatment. Initially, it was available in capsule and oral solution forms, with subsequent approvals for once-daily dosing regimens in 2010[5].

Formulation Evolution

The original capsule formulation of KALETRA has been replaced by a heat-stable tablet formulation, which offers improved bioavailability and does not require administration with food. This change has enhanced patient compliance and convenience[2].

Pharmacokinetics and Bioavailability

The bioavailability of lopinavir is significantly influenced by the presence of ritonavir, which inhibits the CYP3A enzyme and thereby increases lopinavir plasma concentrations. Food intake, particularly high-fat meals, can also increase the bioavailability of lopinavir by up to 130% compared to fasting conditions[1].

Market Positioning

KALETRA has been a critical component of HIV treatment regimens, often used in combination with other antiretroviral drugs. Its market position has been influenced by its efficacy, safety profile, and the evolution of treatment guidelines.

Competition in the HIV Market

The HIV treatment market is highly competitive, with numerous antiretroviral therapies available. KALETRA competes with other protease inhibitors and combination therapies. The market dynamics are driven by factors such as treatment efficacy, side effect profiles, and patient compliance.

Pricing and Access

The pricing of KALETRA has been a subject of interest, particularly in the context of antitrust regulations. Abbott, the manufacturer, has faced scrutiny over pricing strategies, which have impacted market share and patient access[3].

Financial Trajectory

Revenue and Sales

KALETRA has been a significant revenue generator for Abbott. The drug's financial performance has been influenced by its market share, pricing strategies, and the overall demand for HIV treatments. Despite competition, KALETRA has maintained a strong position due to its established efficacy and safety profile.

Impact of Generic Competition

The expiration of patents and the introduction of generic versions of lopinavir/ritonavir have posed challenges to KALETRA's market dominance. Generic competition has led to price reductions and increased access to the drug, particularly in developing countries.

Regulatory and Antitrust Considerations

KALETRA's market dynamics have been shaped by regulatory and antitrust considerations. For instance, antitrust actions have required divestitures in related markets to maintain competition, which indirectly affects the pricing and availability of KALETRA[3].

Use in Special Populations

Pregnancy and Lactation

KALETRA's use in pregnancy is subject to careful consideration due to the potential risks associated with the oral solution, which contains alcohol and propylene glycol. However, the drug is not contraindicated in pregnancy, and its benefits often outweigh the risks[2].

Pediatric Use

The drug is also used in pediatric patients, with dosing recommendations adjusted according to age and weight. The heat-stable tablet formulation has improved the ease of administration in this population.

Safety and Toxicity

KALETRA has a well-documented safety profile, with common side effects including gastrointestinal disturbances and lipid abnormalities. The drug is not mutagenic or clastogenic, and long-term studies have shown no significant effects on fertility in animal models[2].

Conclusion

KALETRA has been a cornerstone in HIV treatment since its approval, with its market dynamics influenced by formulation changes, pharmacokinetics, and regulatory considerations. The financial trajectory of the drug has been marked by significant revenue generation, despite challenges from generic competition and antitrust actions.

Key Takeaways

• Formulation Evolution: From capsules to heat-stable tablets, improving bioavailability and patient compliance.
• Pharmacokinetics: Ritonavir enhances lopinavir bioavailability; food intake, especially high-fat meals, increases bioavailability.
• Market Positioning: Critical component of HIV treatment regimens, competing with other antiretroviral therapies.
• Financial Performance: Significant revenue generator, impacted by generic competition and antitrust actions.
• Regulatory Considerations: Antitrust actions and special population use guidelines shape market dynamics.

FAQs

What is KALETRA used for?

KALETRA is used in the treatment of HIV-1 infection, often in combination with other antiretroviral drugs.

How has the formulation of KALETRA changed over time?

The original capsule formulation has been replaced by a heat-stable tablet formulation, which does not require administration with food and offers improved bioavailability.

How does food intake affect the bioavailability of KALETRA?

High-fat meals can increase the bioavailability of lopinavir by up to 130% compared to fasting conditions.

What are the common side effects of KALETRA?

Common side effects include gastrointestinal disturbances and lipid abnormalities.

Is KALETRA safe for use during pregnancy?

KALETRA can be used during pregnancy, but the oral solution is not recommended due to its alcohol and propylene glycol content.

Sources

1. FDA Label for KALETRA: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021226s030lbl.pdf
2. ClinicalInfo.HIV.Gov - Lopinavir/Ritonavir (Kaletra): https://clinicalinfo.hiv.gov/en/guidelines/perinatal/safety-toxicity-arv-agents-protease-inhibitors-lopinavir-ritonavir-kaletra
3. Antitrust Health Care Chronicle - February 2009: https://www.wsgr.com/attorneys/BIOS/PDFs/rucker0209.pdf
4. FDA Label for KALETRA (2016): https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021251s052_021906s046lbl.pdf
5. Abbott Receives FDA Approval for Once-Daily Dosing of Kaletra: https://www.prnewswire.com/news-releases/abbott-receives-fda-approval-for-once-daily-dosing-of-kaletra-r-lopinavir--ritonavir-for-treatment-experienced-patients-92318364.html