Presented By Facilitated By

ALBIN JOSE.V DR. SHIVALINGE GOWDA K.P.M.Pharm- I H.O.D & Associate Professor

Dept.Of Pharmacology Dept.Of Pharmacology

PESCP PESCP04/15/20231

EVALUATION SEMINAR ONMOLECULAR MECHANISMS OF FDA APPROVED DRUGS

IN 2014

04/15/2023

FDA APPROVED DRUGS IN 2014

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1. Dyloject  - Diclofenac sodium Injection

2.Namzaric   - Donepezil and memantine

3.Saxenda  - Liraglutide Injection

4.Opdivo  - Nivolumab Injection

5.Rapivab - Peramivir Injection

6.Zerbaxa - Ceftolozane and tazobactam Injection

7.Lynparza - Olaparib Capsules

8.Viekira Pak - Ombitasvir/Paritaprevir/Ritonavir with

Dasabuvir Tablets

9.Xtoro  -Finafloxacin Otic Suspension

10.Signifor LAR - Pasireotide for Injectable Suspension

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11.Gardasil 9 - Human papillomavirus 9-valent vaccine,

recombinant Injection

12.Blincyto - Blinatumomab Injection

13.Kitabis Pak  - Tobramycin Inhalation Solution

14.Onexton - Benzoyl peroxide and clindamycin phosphate

Gel

15.Hysingla ER - Hydrocodone bitartrate Extended-Release

Tablets

16.Lemtrada - Alemtuzumab Injection

17.Xigduo XR  - Dapagliflozin and metformin hydrochloride

Extended-Release Tablets

18.Trumenba - Meningococcal group B vaccine

19.Obizur -Antihemophilic factor (recombinant)

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1. Dyloject -Diclofenac sodium Injection

Company: Javelin Pharmaceuticals, Inc.

Approved indication: Pain

Diclofenac sodium injection

It is an intravenous non-steroidal anti-inflammatory drug

(NSAID)

for the management of acute moderate-to-severe pain

in adults.

Molecular Mechanism

1. Inhibition of prostaglandin synthesis by inhibition of 

cyclooxygenase (COX)

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2. Namzaric -Donepezil and Memantine Company: Actavis plc and Adamas Pharmaceuticals

Inc.  Approved indication : Alzheimer's Disease

Molecular Mechanism1. Memantine hydrochloride - NMDA receptor antagonist 2. Donepezil hydrochloride -acetylcholinesterase inhibitor.3. Saxenda -Liraglutide Injection Company: Novo Nordisk Inc.

Approved indication : Obesity Liraglutide is a once-daily dose Glucagon- peptide-1 (GLP-1) analogue for the

treatment of obesity.

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4. Opdivo - Nivolumab Injection Company: Bristol-Myers Squibb Company

Approved indication: Melanoma – Metastatic Nivolumab is a programmed death receptor-1 (PD-1) blocking antibody for the treatment of advanced melanoma.Molecular mechanism Human IgG4 PD-1 immune checkpoint inhibitor “Nivolumab for treatment of malignant melanoma.5. Rapivab -Peramivir Injection Company: BioCryst Pharmaceuticals, Inc.

Approved indication: Influenza

Peramivir is an influenza virus neuraminidase inhibitor Indicated for the treatment of acute uncomplicated influenza in

adults. 

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Mechanism of Action: Peramivir is a cyclopentane analogue It competitively binds to the active site of the influenza virus neuraminidase. Peramivir inhibits the neuraminidase activity of several strains of influenza A and

B viruses, including H1N1 influenza A (swine influenza).

6. Zebra -Ceftolozane and Tazobactam Injection

Company: Cubist Pharmaceuticals, Inc. Approved indication: Intraabdominal Infection, Urinary Tract Infection

Ceftolozane and Tazobactam is a cephalosporin and beta-lactamase inhibitor combination for the treatment of complicated intra-abdominal infections (cIAI) and complicated urinary tract infections (cUTI).

Molecular mechanism

Ceftolozane-Inhibit the cell wall synthesis.

Tazobactum-Beta-lactamase inhibitor.

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7.Lynparza-Olaparib Capsules

Company: AstraZeneca Approved indication: Ovarian Cancer

Mechanism of Action:

Poly adenosine 5’-diphospho ribose polymerase (PARP) family inhibitor PARP-1 PARP- 2  PARP-3.

8. Viekira Pak -Ombitasvir/Paritaprevir/Ritonavir with Dasabuvir Tablets

Company: AbbVie Inc. Approved indication: Chronic Hepatitis C

Viekira Pak for the treatment of patients with genotype 1 chronic hepatitis C virus (HCV) infection.

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Mechanism of actionOmbitasvir - NS5A inhibitor with potent pangenotypic picomolar

antiviral activityParitaprevir - Inhibitor of the NS3/4A serine proteaseRitonavir – Potent inhibitor of CYP3A4 enzymesDasabuvir - Nonnucleoside NS5B polymerase inhibitor and also used

for pharmacologic booster paritaprevir9. Soolantra -Ivermectin Cream Company: Galderma Laboratories, L.P.

Approved indication: Acne Rosacea Lvermectin is a topical antiparasitic with anti-inflammatory properties

for the treatment of rosacea potentially caused by the microscopic skin mite Demodex folliculorum.

Molecular mechanism Anthelmintic drug- Inhibiting neuronal activity and muscular

contractility in arthropods and nematodes By activating glutamate-gated chloride channels (GluClRs) at

nanomolar concentrations

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10.Xtoro -Finafloxacin Otic Suspension Company: Alcon Laboratories, Inc. Approved indication : Otitis ExternaFinafloxacin Otic suspension is a fluoroquinolone

antimicrobial for the treatment of acute otitis externa, commonly known as swimmer’s ear.

Molecular mechanism Quinolones-Inhibit the enzyme bacterial DNA

gyrase.11.Signifor LAR -Pasireotide for Injectable

Suspension Company: Novartis

Approved indication: Acromegaly Pasireotide is a long acting a somatostatin analog

formulation for the treatment of patients with acromegaly.

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Molecular mechanism1. Pasireotide activates somatostatin receptors,

exhibiting a much higher binding affinity for Somatostatin receptors 1, 3, and 5 than octreotide

in vitro, as well as a comparable binding affinity for somatostatin receptor 2. The binding and activation of the somatostatin

receptors causes inhibition of ACTH secretion and results in reduced cortisol secretion in

Cushing's disease patients. Also this agent is more

potent than somatostatin in inhibiting the release of human growth hormone (HGH),

glucagon, and insulin.

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12.Gardasil 9 -Human papillomavirus 9-valent vaccine,

recombinant Injection

Company: Merck & Co., Inc.

Approved indication: Human Papillomavirus

Prophylaxis

Human papillomavirus 9-valent vaccine, recombinant) is a 9-

valent HPV vaccine for the prevention of cervical, vulvar,

vaginal, and anal cancers caused by HPV types 6, 11, 16, 18,

31, 33, 45, 52 and 58.

13.Blincyto -Blinatumomab Injection

Company: Amgen Inc.

Approved indication: Acute Lymphoblastic

Leukemia

Blinatumomab is a bispecific CD19-directed CD3 T-cell engager

indicated for the treatment of Philadelphia chromosome-

negative relapsed or refractory B-cell precursor acute

lymphoblastic leukemia (ALL).

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Molecular mechanism A molecule of Blinatumomab combines two binding sites:  CD3 site for T cells and CD19 site for the target B cells. CD3 is part of the T cell receptor. The drug works by linking these two cell types  activating the T cell to exert cytotoxic activity on the target

cell.14.Kitabis Pak -Tobramycin Inhalation Solution Company: PulmoFlow, Inc.

Approved indication: Cystic Fibrosis Tobramycin is an aminoglycoside inhalation solution co-

packaged with a PARI LC PLUS® Reusable Nebulizer for the management of cystic fibrosis.

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Molecular mechanism Tobramycin binding to a site on the

bacterial 30S and 50S ribosome, preventing formation of the 70S complex. As a result, mRNA cannot be translated into protein

and cell death .15.Onexton-Benzoyl peroxide and Clindamycin

phosphate Gel Company: Valeant Pharmaceuticals

International, Inc. Approved indication: Acne

Benzoyl peroxide and Clindamycin phosphate is an antimicrobial and lincosamide antibacterial combination for the once-daily topical treatment of acne vulgaris

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Molecular mechanismClindamycin: It is a lincosamide antibacterial.  Benzoyl Peroxide: Benzoyl peroxide is an oxidizing

agent with bacteriocidal and keratolytic effects, but the precise mechanism of action is unknown.

16.Hysingla ER-Hydrocodone bitartrate Extended-

Release Tablets Company: Purdue Pharma L.P.

Approved indication: Chronic Pain Hydrocodone is a single-entity (without

acetaminophen) extended-release opioid analgesic for around-the-clock management of moderate to severe chronic pain.

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Molecular mechanism As a narcotic, Hydrocodone relieves pain by binding to Opioid

receptors in the CNS. It acts primarily on μ-opioid receptors, with about six times lesser

affinity to δ-opioid receptors. In blood, 20–50% of hydrocodone is bound to protein.

17.Lemtrada-Alemtuzumab Injection

Company: Genzyme Approved indication: Multiple Sclerosis

Alemtuzumab is a CD52-directed cytolytic monoclonal antibody indicated for the treatment of relapsing forms of multiple sclerosis (MS).

Molecular mechanism Alemtuzumab is a humanized mAb, which targets the surface

molecule CD52 on all T cell populations and other cellular components of the immune system such as thymocytes, B cells, and monocytes.

Alemtuzumab, which is administered intravenously, depletes T as well as B lymphocyte populations for extended periods.

Adverse effects in MS patients such as thyroid disorders and

idiopathic thrombocytopenic purpura.

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18.Xigduo XR -Dapagliflozin and Metformin hydrochloride Extended-Release Tablets

Company: AstraZeneca Approved indication: Diabetes Type 2

Xigduo XR (Dapagliflozin and Metformin hydrochloride)

It is a once-daily sodium-glucose cotransporter 2 (SGLT2) inhibitor and biguanide combination for the treatment of type 2 diabetes.

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Molecular mechanism Dapagliflozin – Inhibits subtype 2 of the sodium-glucose transport

proteins (SGLT2) which are responsible for at least 90% of the

glucose reabsorption in the kidney. Blocking this transporter mechanism causes blood glucose to be

eliminated through the urine.Metformin Metformin decreases hyperglycemia primarily by suppressing

glucose production by the liver (hepatic gluconeogenesis). 19.Trumenba -meningococcal group B vaccine Company: Pfizer Inc.

Approved indication: Meningococcal Meningitis Prophylaxis

Trumenba (Meningococcal group B vaccine) is indicated for active immunization to prevent invasive disease caused by Neisseria

meningitidis serogroup B in adolescents and young adults.